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Acetazolamide Interactions, Mechanism

Acetazolamide Interactions/Acetazolamide 500mg Oral Tablet/Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Acetazolamide and methazolamide are carbonic anhydrase inhibitors used as diuretics and in the therapy of glaucoma. Both acetazolamide and methazolamide have been linked to rare cases of clinically apparent drug-induced liver disease.

Mechanism of Action

The anticonvulsant activity of Acetazolamide may depend on direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. This leads to alkaline urine and an increase in the excretion of bicarbonate, sodium, potassium, and water.

Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Indication of Acetazolamide

  • For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma
  • For adjunctive treatment of edema due to congestive heart failure or drug-induced edema.
  • Glaucoma
  • Acute Mountain Sickness
  • Hydrocephalus
  • Epilepsy
  • Edema
  • Hypokalemic Periodic Paralysis
  • Mountain Sickness / Altitude Sickness
  • Pseudotumor Cerebri
  • Seizure Prevention
  • For the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent.

Therapeutic Uses

  • Anticonvulsants; Carbonic Anhydrase Inhibitors; Diuretics
  • Carbonic anhydrase inhibitors are indicated primarily as adjuncts to other agents in the treatment of open-angle (chronic simple) glaucoma and secondary glaucoma, and to lower intraocular pressure prior to surgery for some types of glaucoma.
  • Acetazolamide is used to lower intraocular pressure in the treatment of malignant (ciliary block) glaucoma, which may occur after inflammation surgery, trauma, or use of miotics. /NOT included in US product labeling/
  • Acetazolamide is indicated as an adjunct to other anticonvulsants in the management of absence seizures (petit mal), generalized tonic-clonic seizures (grand mal), mixed seizure patterns. It may be especially useful for intermittent therapy in females who experience increased seizure activity at the time of menstruation.
  • Oral acetazolamide is indicated to decrease the incidence and/or severity of symptoms (such as headache, nausea, shortness of breath, dizziness, drowsiness, and fatigue) associated with acute altitude sickness in mountain climbers who are attempting rapid ascent and in those who are very susceptible to altitude sickness despite gradual ascent. Gradual ascent is desirable for the prevention of acute altitude sickness even when acetazolamide is used. However, prompt descent may still be necessary if severe manifestations of acute altitude sickness, such as pulmonary edema or cerebral edema, occur.
  • Acetazolamide is used to treat both the hypokalemic and hyperkalemic forms of familial periodic paralysis. It terminates the acute attacks and, with chronic use, prevents their recurrence. It may be the drug of choice in the hypokalemic form of the condition.
  • Parenteral acetazolamide is used to produce a forced alkaline diuresis as a method of increasing the elimination of certain weakly acidic medications.
  • Oral acetazolamide is used to alkalinize the urine as a means of preventing the occurrence or recurrence of uric acid renal stones, especially in patients receiving uricosuric antigout agents, or of cysteine renal stones.
  • Acetazolamide has also been used to prevent or counteract metabolic alkalosis, including that which may occur following open-heart surgery; however, it is no longer used for these indications.
  • Acetazolamide has also been used as a diuretic in the treatment of edema due to congestive heart disease and drug-induced edema. However, it has been replaced by newer diuretics for these indications
  • A placebo-controlled study of the therapy of acute altitude sickness in 12 mountain climbers, 6 of whom were given 250 mg of oral acetazolamide every 8 hr for 2 doses, is reported. After 24 hr, the patients treated with acetazolamide were asymptomatic, whereas those given the placebo still had acute altitude sickness. The alveolar to arterial oxygen pressure difference decor slightly over 24 hr in the acetazolamide group but incr slightly in the placebo group. Acetazolamide improved the arterial partial oxygen pressure over 24 hr when compared with placebo. It was concluded that in established cases of acute altitude sickness, treatment with acetazolamide relieves symptoms, improves arterial oxygenation, and prevents further impairment of pulmonary gas exchange.

Contraindications of Acetazolamide

  • Hyperchloremic acidosis
  • Hypokalemia (low blood potassium)
  • Hyponatremia (low blood sodium)
  • Adrenal insufficiency
  • Impaired kidney function
  • Hypersensitivity to acetazolamide or other sulfonamides.
  • Marked liver disease or impairment of liver function, including cirrhosis because of the risk of development of hepatic encephalopathy. Acetazolamide decreases ammonia clearance
  • type 1 diabetes mellitus
  • a condition where the adrenal glands produce less hormones called Addison’s disease
  • a type of joint disorder due to excess uric acid in the blood called gout
  • respiratory acidosis, an acid-base disorder
  • a blood disorder
  • decreased lung function
  • liver problems
  • severe liver disease
  • renal tubular acidosis
  • recurrent calcium-containing kidney stones
  • decreased kidney function
  • hyperchloremic acidosis

Dosage of Acetazolamide

Strengths: 500 mg; 125 mg; 250 mg

Edema

  • Initial dose: 250 to 375 mg orally/IV once a day
  • If after initial response there is a lack of response, hold therapy for a day
  • Maintenance dose: One dose every other day or once a day for 2 days alternating with a day of rest

Acute Mountain Sickness

  • 500 to 1000 mg orally per day in divided doses
  • Guideline dose: 125 mg orally twice a day
  • AMS Treatment: Guideline dose: 250 mg orally twice a day
  • May use immediate-release or extended-release as appropriate for Acute Mountain Sickness (AMS)/High Altitude Cerebral Edema (HACE) Prevention

Glaucoma

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Glaucoma (Open Angle)

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Seizure Prophylaxis

  • Initial dose: 8 to 30 mg/kg orally/IV in divided doses
  • Range: 375 to 1000 mg per day
  • Initial dose for patients on other anticonvulsants: 250 mg orally/IV once a day

Pediatric Dose

Acute Mountain Sickness

12 years or older:

  • Extended-release capsules: 500 mg orally once or twice a day
  • Guideline dose (immediate-release): 2.5 mg/kg orally every 12 hours
  • Maximum: 125 mg per dose

Glaucoma

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Doses in excess of 1 g/24 hour generally do not produce increased effects.

Glaucoma (Open Angle)

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day

Side Effects of Acetazolamide

The most Common

  • paresthesias, “tingling” feeling in the extremities,
  • some loss of appetite,
  • polyuria,
  • occasional drowsiness,
  • confusion and photosensitivity
  • papular or erythematous skin eruptions,
  • nausea,
  • acidosis and blood dyscrasias.
  • myopia, malaise syndrome,
  • fatigue,
  • anorexia,
  • loss of weight,
  • depression and loss of libido;
  • gastrointestinal distress,
  • elevated blood urate,
  • acute gouty arthritis skin rashes and hair loss or excess growth of hair.

Common 

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of too much acid in the blood (acidosis) like confusion; fast breathing; fast heartbeat; a heartbeat that does not feel normal; very bad stomach pain, upset stomach, or throwing up; feeling very sleepy; shortness of breath; or feeling very tired or weak.
  • Signs of electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, seizures, not hungry, or very bad upset stomach or throwing up.
  • Change in eyesight.
  • Change in hearing.
  • Ringing in ears.

Rare

  • Paresthesias, hearing dysfunction or tinnitus, anorexia, altered taste, nausea, vomiting, diarrhea, polyuria, drowsiness, confusion.
  • A burning, numbness, or tingling feeling that is not normal.
  • Pain when passing urine or blood in the urine.
  • Not able to pass urine or change in how much urine is passed.
  • Muscle weakness.
  • Change in balance.
  • Trouble moving around.
  • Upset stomach or throwing up.
  • Change in taste.
  • Diarrhea.
  • Not hungry.
  • Blurred eyesight.
  • Feeling dizzy, sleepy, tired, or weak.
  • Headache.
  • Flushing.
  • Feeling nervous and excitable.

Drug Interactions of Acetazolamide

View interaction reports for acetazolamide and the medicines listed below.

  • diphenhydramine
  • CoQ10 ubiquinone
  • duloxetine
  • Fish Oil (omega-3 polyunsaturated fatty acids)
  • furosemide
  • pregabalin
  • esomeprazole
  • acetaminophen / hydrocodone
  • acetaminophen
  • albuterol
  • magnesium salicylate
  • metformin
  • methazolamide
  • dichlorphenamide
  • dofetilide
  • dronedarone
  • droperidol
  • citalopram
  • clobazam
  • clonazepam
  • clorazepate
  • clozapine
  • corticorelin
  • corticotropin
  • cortisone
  • montelukast
  • levothyroxine
  • topiramate
  • acetaminophen
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D2 (ergocalciferol)
  • Vitamin D3 (cholecalciferol)
  • ondansetron
  • cetirizine

Pregnancy Category

  • US FDA pregnancy category –  C
  • Pregnancy category – B3 in Australia

Pregnancy

Acetazolamide is pregnancy category B3 in Australia, which means that studies in rats, mice and rabbits in which acetazolamide was given intravenously or orally caused an increased risk of fetal malformations, including defects of the limbs.[rx] Despite this, there is insufficient evidence from studies in humans to either support or discount this evidence.[rx]

Lactation

Limited data are available on the effects of nursing mothers taking acetazolamide. Therapeutic doses create low levels of breast milk and are not expected to cause problems in infants.[rx]

Before taking acetazolamide,

  • tell your doctor and pharmacist if you are allergic to acetazolamide, sulfa drugs, diuretics (‘water pills’), or any other drugs.
  • tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially amphetamines, aspirin, cyclosporine (Neoral, Sandimmune), medications for depression or irregular heartbeat, diflunisal (Dolobid), digoxin (Lanoxin), diuretics (‘water pills’), lithium (Eskalith, Lithobid), phenobarbital, primidone (Mysoline), and vitamins.
  • tell your doctor if you have or have ever had heart, liver, or kidney disease; or diabetes.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking acetazolamide, call your doctor immediately.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking acetazolamide.
  • you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how this drug affects you.
  • remember that alcohol can add to the drowsiness caused by this drug.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Acetazolamide may make your skin sensitive to sunlight.

References

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Acetazolamide Side Effects – Uses, Indications, Warning

Acetazolamide Side Effects/Acetazolamide 500mg Oral Tablet/Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Acetazolamide and methazolamide are carbonic anhydrase inhibitors used as diuretics and in the therapy of glaucoma. Both acetazolamide and methazolamide have been linked to rare cases of clinically apparent drug-induced liver disease.

Mechanism of Action

The anticonvulsant activity of Acetazolamide may depend on direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. This leads to alkaline urine and an increase in the excretion of bicarbonate, sodium, potassium, and water.

Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Indication of Acetazolamide

  • For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma
  • For adjunctive treatment of edema due to congestive heart failure or drug-induced edema.
  • Glaucoma
  • Acute Mountain Sickness
  • Hydrocephalus
  • Epilepsy
  • Edema
  • Hypokalemic Periodic Paralysis
  • Mountain Sickness / Altitude Sickness
  • Pseudotumor Cerebri
  • Seizure Prevention
  • For the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent.

Therapeutic Uses

  • Anticonvulsants; Carbonic Anhydrase Inhibitors; Diuretics
  • Carbonic anhydrase inhibitors are indicated primarily as adjuncts to other agents in the treatment of open-angle (chronic simple) glaucoma and secondary glaucoma, and to lower intraocular pressure prior to surgery for some types of glaucoma.
  • Acetazolamide is used to lower intraocular pressure in the treatment of malignant (ciliary block) glaucoma, which may occur after inflammation surgery, trauma, or use of miotics. /NOT included in US product labeling/
  • Acetazolamide is indicated as an adjunct to other anticonvulsants in the management of absence seizures (petit mal), generalized tonic-clonic seizures (grand mal), mixed seizure patterns. It may be especially useful for intermittent therapy in females who experience increased seizure activity at the time of menstruation.
  • Oral acetazolamide is indicated to decrease the incidence and/or severity of symptoms (such as headache, nausea, shortness of breath, dizziness, drowsiness, and fatigue) associated with acute altitude sickness in mountain climbers who are attempting rapid ascent and in those who are very susceptible to altitude sickness despite gradual ascent. Gradual ascent is desirable for the prevention of acute altitude sickness even when acetazolamide is used. However, prompt descent may still be necessary if severe manifestations of acute altitude sickness, such as pulmonary edema or cerebral edema, occur.
  • Acetazolamide is used to treat both the hypokalemic and hyperkalemic forms of familial periodic paralysis. It terminates the acute attacks and, with chronic use, prevents their recurrence. It may be the drug of choice in the hypokalemic form of the condition.
  • Parenteral acetazolamide is used to produce a forced alkaline diuresis as a method of increasing the elimination of certain weakly acidic medications.
  • Oral acetazolamide is used to alkalinize the urine as a means of preventing the occurrence or recurrence of uric acid renal stones, especially in patients receiving uricosuric antigout agents, or of cysteine renal stones.
  • Acetazolamide has also been used to prevent or counteract metabolic alkalosis, including that which may occur following open-heart surgery; however, it is no longer used for these indications.
  • Acetazolamide has also been used as a diuretic in the treatment of edema due to congestive heart disease and drug-induced edema. However, it has been replaced by newer diuretics for these indications
  • A placebo-controlled study of the therapy of acute altitude sickness in 12 mountain climbers, 6 of whom were given 250 mg of oral acetazolamide every 8 hr for 2 doses, is reported. After 24 hr, the patients treated with acetazolamide were asymptomatic, whereas those given the placebo still had acute altitude sickness. The alveolar to arterial oxygen pressure difference decor slightly over 24 hr in the acetazolamide group but incr slightly in the placebo group. Acetazolamide improved the arterial partial oxygen pressure over 24 hr when compared with placebo. It was concluded that in established cases of acute altitude sickness, treatment with acetazolamide relieves symptoms, improves arterial oxygenation, and prevents further impairment of pulmonary gas exchange.

Contraindications of Acetazolamide

  • Hyperchloremic acidosis
  • Hypokalemia (low blood potassium)
  • Hyponatremia (low blood sodium)
  • Adrenal insufficiency
  • Impaired kidney function
  • Hypersensitivity to acetazolamide or other sulfonamides.
  • Marked liver disease or impairment of liver function, including cirrhosis because of the risk of development of hepatic encephalopathy. Acetazolamide decreases ammonia clearance
  • type 1 diabetes mellitus
  • a condition where the adrenal glands produce less hormones called Addison’s disease
  • a type of joint disorder due to excess uric acid in the blood called gout
  • respiratory acidosis, an acid-base disorder
  • a blood disorder
  • decreased lung function
  • liver problems
  • severe liver disease
  • renal tubular acidosis
  • recurrent calcium-containing kidney stones
  • decreased kidney function
  • hyperchloremic acidosis

Dosage of Acetazolamide

Strengths: 500 mg; 125 mg; 250 mg

Edema

  • Initial dose: 250 to 375 mg orally/IV once a day
  • If after initial response there is a lack of response, hold therapy for a day
  • Maintenance dose: One dose every other day or once a day for 2 days alternating with a day of rest

Acute Mountain Sickness

  • 500 to 1000 mg orally per day in divided doses
  • Guideline dose: 125 mg orally twice a day
  • AMS Treatment: Guideline dose: 250 mg orally twice a day
  • May use immediate-release or extended-release as appropriate for Acute Mountain Sickness (AMS)/High Altitude Cerebral Edema (HACE) Prevention

Glaucoma

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Glaucoma (Open Angle)

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Seizure Prophylaxis

  • Initial dose: 8 to 30 mg/kg orally/IV in divided doses
  • Range: 375 to 1000 mg per day
  • Initial dose for patients on other anticonvulsants: 250 mg orally/IV once a day

Pediatric Dose

Acute Mountain Sickness

12 years or older:

  • Extended-release capsules: 500 mg orally once or twice a day
  • Guideline dose (immediate-release): 2.5 mg/kg orally every 12 hours
  • Maximum: 125 mg per dose

Glaucoma

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Doses in excess of 1 g/24 hour generally do not produce increased effects.

Glaucoma (Open Angle)

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day

Side Effects of Acetazolamide

The most Common

  • paresthesias, “tingling” feeling in the extremities,
  • some loss of appetite,
  • polyuria,
  • occasional drowsiness,
  • confusion and photosensitivity
  • papular or erythematous skin eruptions,
  • nausea,
  • acidosis and blood dyscrasias.
  • myopia, malaise syndrome,
  • fatigue,
  • anorexia,
  • loss of weight,
  • depression and loss of libido;
  • gastrointestinal distress,
  • elevated blood urate,
  • acute gouty arthritis skin rashes and hair loss or excess growth of hair.

Common 

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of too much acid in the blood (acidosis) like confusion; fast breathing; fast heartbeat; a heartbeat that does not feel normal; very bad stomach pain, upset stomach, or throwing up; feeling very sleepy; shortness of breath; or feeling very tired or weak.
  • Signs of electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, seizures, not hungry, or very bad upset stomach or throwing up.
  • Change in eyesight.
  • Change in hearing.
  • Ringing in ears.

Rare

  • Paresthesias, hearing dysfunction or tinnitus, anorexia, altered taste, nausea, vomiting, diarrhea, polyuria, drowsiness, confusion.
  • A burning, numbness, or tingling feeling that is not normal.
  • Pain when passing urine or blood in the urine.
  • Not able to pass urine or change in how much urine is passed.
  • Muscle weakness.
  • Change in balance.
  • Trouble moving around.
  • Upset stomach or throwing up.
  • Change in taste.
  • Diarrhea.
  • Not hungry.
  • Blurred eyesight.
  • Feeling dizzy, sleepy, tired, or weak.
  • Headache.
  • Flushing.
  • Feeling nervous and excitable.

Drug Interactions of Acetazolamide

View interaction reports for acetazolamide and the medicines listed below.

  • diphenhydramine
  • CoQ10 ubiquinone
  • duloxetine
  • Fish Oil (omega-3 polyunsaturated fatty acids)
  • furosemide
  • pregabalin
  • esomeprazole
  • acetaminophen / hydrocodone
  • acetaminophen
  • albuterol
  • magnesium salicylate
  • metformin
  • methazolamide
  • dichlorphenamide
  • dofetilide
  • dronedarone
  • droperidol
  • citalopram
  • clobazam
  • clonazepam
  • clorazepate
  • clozapine
  • corticorelin
  • corticotropin
  • cortisone
  • montelukast
  • levothyroxine
  • topiramate
  • acetaminophen
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D2 (ergocalciferol)
  • Vitamin D3 (cholecalciferol)
  • ondansetron
  • cetirizine

Pregnancy Category

  • US FDA pregnancy category –  C
  • Pregnancy category – B3 in Australia

Pregnancy

Acetazolamide is pregnancy category B3 in Australia, which means that studies in rats, mice and rabbits in which acetazolamide was given intravenously or orally caused an increased risk of fetal malformations, including defects of the limbs.[rx] Despite this, there is insufficient evidence from studies in humans to either support or discount this evidence.[rx]

Lactation

Limited data are available on the effects of nursing mothers taking acetazolamide. Therapeutic doses create low levels of breast milk and are not expected to cause problems in infants.[rx]

Before taking acetazolamide,

  • tell your doctor and pharmacist if you are allergic to acetazolamide, sulfa drugs, diuretics (‘water pills’), or any other drugs.
  • tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially amphetamines, aspirin, cyclosporine (Neoral, Sandimmune), medications for depression or irregular heartbeat, diflunisal (Dolobid), digoxin (Lanoxin), diuretics (‘water pills’), lithium (Eskalith, Lithobid), phenobarbital, primidone (Mysoline), and vitamins.
  • tell your doctor if you have or have ever had heart, liver, or kidney disease; or diabetes.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking acetazolamide, call your doctor immediately.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking acetazolamide.
  • you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how this drug affects you.
  • remember that alcohol can add to the drowsiness caused by this drug.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Acetazolamide may make your skin sensitive to sunlight.

References

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Acetazolamide 500mg Oral Tablet – Indications, Contraindications

Acetazolamide 500mg Oral Tablet/Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Acetazolamide and methazolamide are carbonic anhydrase inhibitors used as diuretics and in the therapy of glaucoma. Both acetazolamide and methazolamide have been linked to rare cases of clinically apparent drug-induced liver disease.

Mechanism of Action

The anticonvulsant activity of Acetazolamide may depend on direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. This leads to alkaline urine and an increase in the excretion of bicarbonate, sodium, potassium, and water.

Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Indication of Acetazolamide

  • For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma
  • For adjunctive treatment of edema due to congestive heart failure or drug-induced edema.
  • Glaucoma
  • Acute Mountain Sickness
  • Hydrocephalus
  • Epilepsy
  • Edema
  • Hypokalemic Periodic Paralysis
  • Mountain Sickness / Altitude Sickness
  • Pseudotumor Cerebri
  • Seizure Prevention
  • For the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent.

Therapeutic Uses

  • Anticonvulsants; Carbonic Anhydrase Inhibitors; Diuretics
  • Carbonic anhydrase inhibitors are indicated primarily as adjuncts to other agents in the treatment of open-angle (chronic simple) glaucoma and secondary glaucoma, and to lower intraocular pressure prior to surgery for some types of glaucoma.
  • Acetazolamide is used to lower intraocular pressure in the treatment of malignant (ciliary block) glaucoma, which may occur after inflammation surgery, trauma, or use of miotics. /NOT included in US product labeling/
  • Acetazolamide is indicated as an adjunct to other anticonvulsants in the management of absence seizures (petit mal), generalized tonic-clonic seizures (grand mal), mixed seizure patterns. It may be especially useful for intermittent therapy in females who experience increased seizure activity at the time of menstruation.
  • Oral acetazolamide is indicated to decrease the incidence and/or severity of symptoms (such as headache, nausea, shortness of breath, dizziness, drowsiness, and fatigue) associated with acute altitude sickness in mountain climbers who are attempting rapid ascent and in those who are very susceptible to altitude sickness despite gradual ascent. Gradual ascent is desirable for the prevention of acute altitude sickness even when acetazolamide is used. However, prompt descent may still be necessary if severe manifestations of acute altitude sickness, such as pulmonary edema or cerebral edema, occur.
  • Acetazolamide is used to treat both the hypokalemic and hyperkalemic forms of familial periodic paralysis. It terminates the acute attacks and, with chronic use, prevents their recurrence. It may be the drug of choice in the hypokalemic form of the condition.
  • Parenteral acetazolamide is used to produce a forced alkaline diuresis as a method of increasing the elimination of certain weakly acidic medications.
  • Oral acetazolamide is used to alkalinize the urine as a means of preventing the occurrence or recurrence of uric acid renal stones, especially in patients receiving uricosuric antigout agents, or of cysteine renal stones.
  • Acetazolamide has also been used to prevent or counteract metabolic alkalosis, including that which may occur following open-heart surgery; however, it is no longer used for these indications.
  • Acetazolamide has also been used as a diuretic in the treatment of edema due to congestive heart disease and drug-induced edema. However, it has been replaced by newer diuretics for these indications
  • A placebo-controlled study of the therapy of acute altitude sickness in 12 mountain climbers, 6 of whom were given 250 mg of oral acetazolamide every 8 hr for 2 doses, is reported. After 24 hr, the patients treated with acetazolamide were asymptomatic, whereas those given the placebo still had acute altitude sickness. The alveolar to arterial oxygen pressure difference decor slightly over 24 hr in the acetazolamide group but incr slightly in the placebo group. Acetazolamide improved the arterial partial oxygen pressure over 24 hr when compared with placebo. It was concluded that in established cases of acute altitude sickness, treatment with acetazolamide relieves symptoms, improves arterial oxygenation, and prevents further impairment of pulmonary gas exchange.

Contraindications of Acetazolamide

  • Hyperchloremic acidosis
  • Hypokalemia (low blood potassium)
  • Hyponatremia (low blood sodium)
  • Adrenal insufficiency
  • Impaired kidney function
  • Hypersensitivity to acetazolamide or other sulfonamides.
  • Marked liver disease or impairment of liver function, including cirrhosis because of the risk of development of hepatic encephalopathy. Acetazolamide decreases ammonia clearance
  • type 1 diabetes mellitus
  • a condition where the adrenal glands produce less hormones called Addison’s disease
  • a type of joint disorder due to excess uric acid in the blood called gout
  • respiratory acidosis, an acid-base disorder
  • a blood disorder
  • decreased lung function
  • liver problems
  • severe liver disease
  • renal tubular acidosis
  • recurrent calcium-containing kidney stones
  • decreased kidney function
  • hyperchloremic acidosis

Dosage of Acetazolamide

Strengths: 500 mg; 125 mg; 250 mg

Edema

  • Initial dose: 250 to 375 mg orally/IV once a day
  • If after initial response there is a lack of response, hold therapy for a day
  • Maintenance dose: One dose every other day or once a day for 2 days alternating with a day of rest

Acute Mountain Sickness

  • 500 to 1000 mg orally per day in divided doses
  • Guideline dose: 125 mg orally twice a day
  • AMS Treatment: Guideline dose: 250 mg orally twice a day
  • May use immediate-release or extended-release as appropriate for Acute Mountain Sickness (AMS)/High Altitude Cerebral Edema (HACE) Prevention

Glaucoma

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Glaucoma (Open Angle)

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Seizure Prophylaxis

  • Initial dose: 8 to 30 mg/kg orally/IV in divided doses
  • Range: 375 to 1000 mg per day
  • Initial dose for patients on other anticonvulsants: 250 mg orally/IV once a day

Pediatric Dose

Acute Mountain Sickness

12 years or older:

  • Extended-release capsules: 500 mg orally once or twice a day
  • Guideline dose (immediate-release): 2.5 mg/kg orally every 12 hours
  • Maximum: 125 mg per dose

Glaucoma

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Doses in excess of 1 g/24 hour generally do not produce increased effects.

Glaucoma (Open Angle)

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day

Side Effects of Acetazolamide

The most Common

  • paresthesias, “tingling” feeling in the extremities,
  • some loss of appetite,
  • polyuria,
  • occasional drowsiness,
  • confusion and photosensitivity
  • papular or erythematous skin eruptions,
  • nausea,
  • acidosis and blood dyscrasias.
  • myopia, malaise syndrome,
  • fatigue,
  • anorexia,
  • loss of weight,
  • depression and loss of libido;
  • gastrointestinal distress,
  • elevated blood urate,
  • acute gouty arthritis skin rashes and hair loss or excess growth of hair.

Common 

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of too much acid in the blood (acidosis) like confusion; fast breathing; fast heartbeat; a heartbeat that does not feel normal; very bad stomach pain, upset stomach, or throwing up; feeling very sleepy; shortness of breath; or feeling very tired or weak.
  • Signs of electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, seizures, not hungry, or very bad upset stomach or throwing up.
  • Change in eyesight.
  • Change in hearing.
  • Ringing in ears.

Rare

  • Paresthesias, hearing dysfunction or tinnitus, anorexia, altered taste, nausea, vomiting, diarrhea, polyuria, drowsiness, confusion.
  • A burning, numbness, or tingling feeling that is not normal.
  • Pain when passing urine or blood in the urine.
  • Not able to pass urine or change in how much urine is passed.
  • Muscle weakness.
  • Change in balance.
  • Trouble moving around.
  • Upset stomach or throwing up.
  • Change in taste.
  • Diarrhea.
  • Not hungry.
  • Blurred eyesight.
  • Feeling dizzy, sleepy, tired, or weak.
  • Headache.
  • Flushing.
  • Feeling nervous and excitable.

Drug Interactions of Acetazolamide

View interaction reports for acetazolamide and the medicines listed below.

  • diphenhydramine
  • CoQ10 ubiquinone
  • duloxetine
  • Fish Oil (omega-3 polyunsaturated fatty acids)
  • furosemide
  • pregabalin
  • esomeprazole
  • acetaminophen / hydrocodone
  • acetaminophen
  • albuterol
  • magnesium salicylate
  • metformin
  • methazolamide
  • dichlorphenamide
  • dofetilide
  • dronedarone
  • droperidol
  • citalopram
  • clobazam
  • clonazepam
  • clorazepate
  • clozapine
  • corticorelin
  • corticotropin
  • cortisone
  • montelukast
  • levothyroxine
  • topiramate
  • acetaminophen
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D2 (ergocalciferol)
  • Vitamin D3 (cholecalciferol)
  • ondansetron
  • cetirizine

Pregnancy Category

  • US FDA pregnancy category –  C
  • Pregnancy category – B3 in Australia

Pregnancy

Acetazolamide is pregnancy category B3 in Australia, which means that studies in rats, mice and rabbits in which acetazolamide was given intravenously or orally caused an increased risk of fetal malformations, including defects of the limbs.[rx] Despite this, there is insufficient evidence from studies in humans to either support or discount this evidence.[rx]

Lactation

Limited data are available on the effects of nursing mothers taking acetazolamide. Therapeutic doses create low levels of breast milk and are not expected to cause problems in infants.[rx]

Before taking acetazolamide,

  • tell your doctor and pharmacist if you are allergic to acetazolamide, sulfa drugs, diuretics (‘water pills’), or any other drugs.
  • tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially amphetamines, aspirin, cyclosporine (Neoral, Sandimmune), medications for depression or irregular heartbeat, diflunisal (Dolobid), digoxin (Lanoxin), diuretics (‘water pills’), lithium (Eskalith, Lithobid), phenobarbital, primidone (Mysoline), and vitamins.
  • tell your doctor if you have or have ever had heart, liver, or kidney disease; or diabetes.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking acetazolamide, call your doctor immediately.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking acetazolamide.
  • you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how this drug affects you.
  • remember that alcohol can add to the drowsiness caused by this drug.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Acetazolamide may make your skin sensitive to sunlight.

References

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Acetazolamide – Uses, Dosage, Side Effects, Interactions

Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Acetazolamide and methazolamide are carbonic anhydrase inhibitors used as diuretics and in the therapy of glaucoma. Both acetazolamide and methazolamide have been linked to rare cases of clinically apparent drug-induced liver disease.

Mechanism of Action

The anticonvulsant activity of Acetazolamide may depend on direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. This leads to alkaline urine and an increase in the excretion of bicarbonate, sodium, potassium, and water.

Acetazolamide is a sulfonamide derivative with diuretic, antiglaucoma, and anticonvulsant properties. Acetazolamide is a non-competitive inhibitor of carbonic anhydrase, an enzyme found in cells in the proximal tube of the kidney, the eye, and glial cells. Inhibition of this enzyme in the kidney prevents excretion of hydrogen, leading to increased bicarbonate and cation excretion and increased urinary volume, which results in an alkaline diuresis. Acetazolamide reduces the concentration of bicarbonate, resulting in a decreased synthesis of aqueous humor in the eye, thereby lowering intraocular pressure. Although its mechanism of action is unknown, acetazolamide has anti-convulsant properties resulting from indirect effects secondary to metabolic acidosis or direct effects on neuronal transmission. Acetazolamide also produces respiratory stimulant effects in response to changes to both carbon dioxide and oxygen tension levels within the lungs.

Indication of Acetazolamide

  • For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma
  • For adjunctive treatment of edema due to congestive heart failure or drug-induced edema.
  • Glaucoma
  • Acute Mountain Sickness
  • Hydrocephalus
  • Epilepsy
  • Edema
  • Hypokalemic Periodic Paralysis
  • Mountain Sickness / Altitude Sickness
  • Pseudotumor Cerebri
  • Seizure Prevention
  • For the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent.

Therapeutic Uses

  • Anticonvulsants; Carbonic Anhydrase Inhibitors; Diuretics
  • Carbonic anhydrase inhibitors are indicated primarily as adjuncts to other agents in the treatment of open-angle (chronic simple) glaucoma and secondary glaucoma, and to lower intraocular pressure prior to surgery for some types of glaucoma.
  • Acetazolamide is used to lower intraocular pressure in the treatment of malignant (ciliary block) glaucoma, which may occur after inflammation surgery, trauma, or use of miotics. /NOT included in US product labeling/
  • Acetazolamide is indicated as an adjunct to other anticonvulsants in the management of absence seizures (petit mal), generalized tonic-clonic seizures (grand mal), mixed seizure patterns. It may be especially useful for intermittent therapy in females who experience increased seizure activity at the time of menstruation.
  • Oral acetazolamide is indicated to decrease the incidence and/or severity of symptoms (such as headache, nausea, shortness of breath, dizziness, drowsiness, and fatigue) associated with acute altitude sickness in mountain climbers who are attempting rapid ascent and in those who are very susceptible to altitude sickness despite gradual ascent. Gradual ascent is desirable for the prevention of acute altitude sickness even when acetazolamide is used. However, prompt descent may still be necessary if severe manifestations of acute altitude sickness, such as pulmonary edema or cerebral edema, occur.
  • Acetazolamide is used to treat both the hypokalemic and hyperkalemic forms of familial periodic paralysis. It terminates the acute attacks and, with chronic use, prevents their recurrence. It may be the drug of choice in the hypokalemic form of the condition.
  • Parenteral acetazolamide is used to produce a forced alkaline diuresis as a method of increasing the elimination of certain weakly acidic medications.
  • Oral acetazolamide is used to alkalinize the urine as a means of preventing the occurrence or recurrence of uric acid renal stones, especially in patients receiving uricosuric antigout agents, or of cysteine renal stones.
  • Acetazolamide has also been used to prevent or counteract metabolic alkalosis, including that which may occur following open-heart surgery; however, it is no longer used for these indications.
  • Acetazolamide has also been used as a diuretic in the treatment of edema due to congestive heart disease and drug-induced edema. However, it has been replaced by newer diuretics for these indications
  • A placebo-controlled study of the therapy of acute altitude sickness in 12 mountain climbers, 6 of whom were given 250 mg of oral acetazolamide every 8 hr for 2 doses, is reported. After 24 hr, the patients treated with acetazolamide were asymptomatic, whereas those given the placebo still had acute altitude sickness. The alveolar to arterial oxygen pressure difference decor slightly over 24 hr in the acetazolamide group but incr slightly in the placebo group. Acetazolamide improved the arterial partial oxygen pressure over 24 hr when compared with placebo. It was concluded that in established cases of acute altitude sickness, treatment with acetazolamide relieves symptoms, improves arterial oxygenation, and prevents further impairment of pulmonary gas exchange.

Contraindications of Acetazolamide

  • Hyperchloremic acidosis
  • Hypokalemia (low blood potassium)
  • Hyponatremia (low blood sodium)
  • Adrenal insufficiency
  • Impaired kidney function
  • Hypersensitivity to acetazolamide or other sulfonamides.
  • Marked liver disease or impairment of liver function, including cirrhosis because of the risk of development of hepatic encephalopathy. Acetazolamide decreases ammonia clearance
  • type 1 diabetes mellitus
  • a condition where the adrenal glands produce less hormones called Addison’s disease
  • a type of joint disorder due to excess uric acid in the blood called gout
  • respiratory acidosis, an acid-base disorder
  • a blood disorder
  • decreased lung function
  • liver problems
  • severe liver disease
  • renal tubular acidosis
  • recurrent calcium-containing kidney stones
  • decreased kidney function
  • hyperchloremic acidosis

Dosage of Acetazolamide

Strengths: 500 mg; 125 mg; 250 mg

Edema

  • Initial dose: 250 to 375 mg orally/IV once a day
  • If after initial response there is a lack of response, hold therapy for a day
  • Maintenance dose: One dose every other day or once a day for 2 days alternating with a day of rest

Acute Mountain Sickness

  • 500 to 1000 mg orally per day in divided doses
  • Guideline dose: 125 mg orally twice a day
  • AMS Treatment: Guideline dose: 250 mg orally twice a day
  • May use immediate-release or extended-release as appropriate for Acute Mountain Sickness (AMS)/High Altitude Cerebral Edema (HACE) Prevention

Glaucoma

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Glaucoma (Open Angle)

Open-Angle Glaucoma

  • Immediate-release (IR) tablets: 250 to 1000 mg orally per day; amounts over 250 mg should be administered in divided doses
  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Maintenance: Adjust doses individually based on symptomatology and ocular tension; for patients inadequately controlled on ER capsules 1 g/day, may supplement with IR tablets
  • Doses in excess of 1 g/24 hour generally do not produce increased effects

Preoperatively in Closed-Angle Glaucoma

  • Various regimens have been used including 250 mg orally every 4 hours; 250 mg orally twice a day; OR 500 mg orally followed by 125 mg or 250 mg orally every 4 hours

Seizure Prophylaxis

  • Initial dose: 8 to 30 mg/kg orally/IV in divided doses
  • Range: 375 to 1000 mg per day
  • Initial dose for patients on other anticonvulsants: 250 mg orally/IV once a day

Pediatric Dose

Acute Mountain Sickness

12 years or older:

  • Extended-release capsules: 500 mg orally once or twice a day
  • Guideline dose (immediate-release): 2.5 mg/kg orally every 12 hours
  • Maximum: 125 mg per dose

Glaucoma

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day
  • Doses in excess of 1 g/24 hour generally do not produce increased effects.

Glaucoma (Open Angle)

12 years or older

  • Extended-release (ER) capsules: 500 mg orally 2 times a day

Side Effects of Acetazolamide

The most Common

  • paresthesias, “tingling” feeling in the extremities,
  • some loss of appetite,
  • polyuria,
  • occasional drowsiness,
  • confusion and photosensitivity
  • papular or erythematous skin eruptions,
  • nausea,
  • acidosis and blood dyscrasias.
  • myopia, malaise syndrome,
  • fatigue,
  • anorexia,
  • loss of weight,
  • depression and loss of libido;
  • gastrointestinal distress,
  • elevated blood urate,
  • acute gouty arthritis skin rashes and hair loss or excess growth of hair.

Common 

  • Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
  • Signs of too much acid in the blood (acidosis) like confusion; fast breathing; fast heartbeat; a heartbeat that does not feel normal; very bad stomach pain, upset stomach, or throwing up; feeling very sleepy; shortness of breath; or feeling very tired or weak.
  • Signs of electrolyte problems like mood changes, confusion, muscle pain or weakness, a heartbeat that does not feel normal, seizures, not hungry, or very bad upset stomach or throwing up.
  • Change in eyesight.
  • Change in hearing.
  • Ringing in ears.

Rare

  • Paresthesias, hearing dysfunction or tinnitus, anorexia, altered taste, nausea, vomiting, diarrhea, polyuria, drowsiness, confusion.
  • A burning, numbness, or tingling feeling that is not normal.
  • Pain when passing urine or blood in the urine.
  • Not able to pass urine or change in how much urine is passed.
  • Muscle weakness.
  • Change in balance.
  • Trouble moving around.
  • Upset stomach or throwing up.
  • Change in taste.
  • Diarrhea.
  • Not hungry.
  • Blurred eyesight.
  • Feeling dizzy, sleepy, tired, or weak.
  • Headache.
  • Flushing.
  • Feeling nervous and excitable.

Drug Interactions of Acetazolamide

View interaction reports for acetazolamide and the medicines listed below.

  • diphenhydramine
  • CoQ10 ubiquinone
  • duloxetine
  • Fish Oil (omega-3 polyunsaturated fatty acids)
  • furosemide
  • pregabalin
  • esomeprazole
  • acetaminophen / hydrocodone
  • acetaminophen
  • albuterol
  • magnesium salicylate
  • metformin
  • methazolamide
  • dichlorphenamide
  • dofetilide
  • dronedarone
  • droperidol
  • citalopram
  • clobazam
  • clonazepam
  • clorazepate
  • clozapine
  • corticorelin
  • corticotropin
  • cortisone
  • montelukast
  • levothyroxine
  • topiramate
  • acetaminophen
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D2 (ergocalciferol)
  • Vitamin D3 (cholecalciferol)
  • ondansetron
  • cetirizine

Pregnancy Category

  • US FDA pregnancy category –  C
  • Pregnancy category – B3 in Australia

Pregnancy

Acetazolamide is pregnancy category B3 in Australia, which means that studies in rats, mice and rabbits in which acetazolamide was given intravenously or orally caused an increased risk of fetal malformations, including defects of the limbs.[rx] Despite this, there is insufficient evidence from studies in humans to either support or discount this evidence.[rx]

Lactation

Limited data are available on the effects of nursing mothers taking acetazolamide. Therapeutic doses create low levels of breast milk and are not expected to cause problems in infants.[rx]

Before taking acetazolamide,

  • tell your doctor and pharmacist if you are allergic to acetazolamide, sulfa drugs, diuretics (‘water pills’), or any other drugs.
  • tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially amphetamines, aspirin, cyclosporine (Neoral, Sandimmune), medications for depression or irregular heartbeat, diflunisal (Dolobid), digoxin (Lanoxin), diuretics (‘water pills’), lithium (Eskalith, Lithobid), phenobarbital, primidone (Mysoline), and vitamins.
  • tell your doctor if you have or have ever had heart, liver, or kidney disease; or diabetes.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking acetazolamide, call your doctor immediately.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking acetazolamide.
  • you should know that this drug may make you drowsy. Do not drive a car or operate machinery until you know how this drug affects you.
  • remember that alcohol can add to the drowsiness caused by this drug.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Acetazolamide may make your skin sensitive to sunlight.

References

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Is nabumetone stronger than naproxen?

Is nabumetone stronger than naproxen?After 12 weeks of treatment, researchers found that nabumetone was similar in effectiveness to ibuprofen and other NSAIDs when treating osteoarthritis. However, the study found that nabumetone was more effective than the other NSAIDs for rheumatoid arthritis.

/Nabumetone is a naphthyl alkenone and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, and analgesic activities. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthyl acetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone. The formation of thromboxane A2, by thromboxane synthase, is also decreased and results in an inhibition of platelet aggregation.

Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.

Nabumetone is a methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthyl acetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, a cyclooxygenase 2 inhibitor, and a prodrug. It is a methoxynaphthalene and a methyl ketone.

Mechanism of Action

Nabumetone’s active metabolite, 6-MNA, is an inhibitor of both COX-1 and COX-2 although it exhibits some COX-2 selectivity.[label, A178903] Inhibition of COX-1 and COX-2 reduces the conversion of arachidonic acid to PGs and thromboxane (TXA2). This reduction in prostanoid production is the common mechanism that mediates the effects of nabumetone. PGE2 is the primary PG involved in the modulation of nociception.[A179023] It mediates peripheral sensitization through a variety of effects.[T116, A179023] PGE2 activates the Gq-coupled EP1 receptor leading to increased activity of the inositol trisphosphate/phospholipase C pathway. Activation of this pathway releases intracellular stores of calcium which directly reduces action potential threshold and activates protein kinase C (PKC) which contributes to several indirect mechanisms. PGE2 also activates the EP4 receptor, coupled to Gs, which activates the adenylyl cyclase/protein kinase A (AC/PKA) signaling pathway. PKA and PKC both contribute to the potentiation of transient receptor potential cation channel subfamily V member 1 (TRPV1) potentiation, which increases sensitivity to heat stimuli. They also activate tetrodotoxin-resistant sodium channels and inhibit inward potassium currents. PKA further contributes to the activation of the P2X3 purine receptor and sensitization of T-type calcium channels. The activation and sensitization of depolarizing ion channels and inhibition of inward potassium currents serve to reduce the intensity of stimulus necessary to generate action potentials in nociceptive sensory afferents. PGE2 act via EP3 to increase sensitivity to bradykinin and via EP2 to further increase heat sensitivity. Central sensitization occurs in the dorsal horn of the spinal cord and is mediated by the EP2 receptor which couples to Gs. Pre-synaptically, this receptor increases the release of pro-nociceptive neurotransmitters glutamate, CGRP, and substance P. Post-synaptically it increases the activity of AMPA and NMDA receptors and produces inhibition of inhibitory glycinergic neurons. Together these lead to a reduced threshold of activating, allowing low intensity stimuli to generate pain signals. PGI2 is known to play a role via its Gs-coupled IP receptor although the magnitude of its contribution varies. It has been proposed to be of greater importance in painful inflammatory conditions such as arthritis. By limiting sensitization, both peripheral and central, via these pathways NSAIDs can effectively reduce inflammatory pain. PGI2 and PGE2 contribute to acute inflammation via their IP and EP2 receptors.[T116, A179044] Similarly to β adrenergic receptors these are Gs-coupled and mediate vasodilation through the AC/PKA pathway. PGE2 also contributes by increasing leukocyte adhesion to the endothelium and attracts the cells to the site of injury.[T116] PGD2 plays a role in the activation of endothelial cell release of cytokines through its DP1 receptor.[A179044] PGI2 and PGE2 modulate T-helper cell activation and differentiation through IP, EP2, and EP4 receptors which are believed to be an important activity in the pathology of arthritic conditions. By limiting the production of these PGs at the site of injury, NSAIDs can reduce inflammation. PGE2 can cross the blood-brain barrier and act on excitatory Gq EP3 receptors on thermoregulatory neurons in the hypothalamus.[T116] This activation triggers an increase in heat generation and a reduction in heat loss to produce a fever. NSAIDs prevent the generation of PGE2 thereby reducing the activity of these neurons. The adverse effects of NSAIDs stem from the protective and regulatory roles of prostanoids which have been well-characterized.[T116] PGI2 and PGE2 regulate blood flow to the kidney by similar mechanisms to the vasodilation they produce in inflammation. Prevention of this regulation by NSAIDs produces vasoconstriction which limits renal function by reducing blood flow and hydrostatic pressure which drives filtration. PGE2 also regulates gastric protection via EP3 receptors which are, in this location, coupled to Gi which inhibits the AC/PKA pathway. This reduces the secretion of protons by H+/K+ ATPase in parietal cells and increases the secretion of mucus and HCO3– by superficial endothelial cells. Disruption of this protective action by NSAIDs leads to ulceration of the gastric mucosa. Lastly, disruption of PGI2, which opposes platelet aggregation, generation by COX-2 selective agents leads to an imbalance with TXA2 generated by COX-1, which promotes aggregation of platelets, leading to increased risk of thrombosis. Since nabumetone is somewhat COX-2 selective it is thought to promote this imbalance and increase thrombotic risk.

Indications of Nabumetone 

  • Indicated for  Symptomatic relief in rheumatoid arthritis.
  • Symptomatic relief in osteoarthritis.
  • Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.
  • Back Pain
  • Sciatica
  • Muscle Pain
  • Rheumatoid Arthritis
  • Frozen Shoulder

Contraindications of Nabumetone

  • Hypersensitivity to the active substance or to any of the excipients,
  • Nabumetone must not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking acetylsalicylic acid or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
  • Nabumetone is contraindicated in patients with severe hepatic failure.
  • Nabumetone is contraindicated in patients with a history of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
  • Nabumetone is contraindicated in patients with active, or history of recurrent, peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
  • Nabumetone is contraindicated in the third trimester of pregnancy and in nursing mothers.
  • Nabumetone is contraindicated in patients with severe heart failure, and in patients with current cerebrovascular or another hemorrhage.
  • a heart attack
  • chronic heart failure
  • abnormal bleeding in the brain resulting in damage to brain tissue, called a hemorrhagic stroke
  • a blood clot
  • an ulcer from too much stomach acid
  • stomach or intestinal ulcer
  • liver problems
  • bleeding of the stomach or intestines
  • kidney transplant
  • pregnancy
  • a rupture in the wall of the stomach or intestine
  • tobacco smoking
  • increased cardiovascular event risk
  • the time immediately after coronary bypass surgery
  • chronic kidney disease stage 4 (severe)
  • chronic kidney disease stage 5 (failure)
  • kidney disease with likely reduction in kidney function
  • aspirin-exacerbated respiratory disease
  • history of gastric bypass surgery
  • history of kidney donation

Dosage of Nabumetone

  • Strengths: 500 mg; 750 mg; 1000 mg

Osteoarthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Rheumatoid Arthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Renal Dose Adjustments

  • Mild renal dysfunction (CrCl 50 mL/min or greater): No adjustment recommended.

Moderate renal dysfunction (CrCl 30 to 49 mL/min)

  • Initial dose: 750 mg orally once a day
  • Maximum dose: 1500 mg/day

Severe renal dysfunction (CrCl less than 30 mL/min)

  • Initial dose: 500 mg orally once a day
  • Maximum dose: 1000 mg/day

Side Effects of Nabumetone

The Most Common

  • shortness of breath (even with mild exertion);
  • swelling or rapid weight gain;
  • the first sign of any skin rash, no matter how mild;
  • signs of stomach bleeding–bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
  • liver problems–nausea, upper stomach pain, itching, tired feeling, flu-like symptoms, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • kidney problems–little or no urinating, painful or difficult urination, swelling in your feet or ankles, feeling tired or short of breath; or
  • low red blood cells (anemia)–pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet.
  • stomach pain, indigestion, nausea;
  • diarrhea, constipation, gas;
  • swelling in your hands and feet;
  • headache, dizziness;
  • itching, skin rash; or
  • ringing in your ears.

Common

  • Acid or sour stomach
  • belching
  • loss of appetite
  • muscle pain
  • pain in lower back or side
  • pinpoint red spots on skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips or tongue
  • rapid breathing
  • red irritated eyes
  • red skin lesions, often with a purple center
  • redness or other discoloration of skin
  • severe or continuing stomach pain
  • bloated full feeling
  • continuing ringing or buzzing or other unexplained noise in ears
  • excess air or gas in stomach or intestines
  • hearing loss
  • indigestion
  • mild diarrhea
  • passing gas

Rare

  • Increased sweating
  • sleepiness or unusual drowsiness
  • sleeplessness
  • trouble sleeping
  • unable to sleep
  • Bleeding gums
  • blistering, peeling, loosening of skin
  • bloody or black, tarry stools
  • bloody or cloudy urine
  • burning upper abdominal pain
  • changes in vision
  • chest pain
  • chills
  • clay-colored stools
  • general feeling of tiredness or weakness
  • greatly decreased frequency of urination or amount of urine
  • high blood pressure
  • hives or welts
  • increased sensitivity of skin to sunlight
  • increased thirst
  • joint pain, stiffness, or swelling
  • large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs

Drug Interactions of Nabumetone

Common medications that may interact with nabumetone include:

  • All other NSAID drugs except nabumetone
  • ACE inhibitors or ARBs, such as captopril, enalapril, or losartan
  • aminoglycosides, such as gentamicin
  • antibiotics, such as ciprofloxacin, norfloxacin, or vancomycin
  • anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
  • antidepressants, such as citalopram, escitalopram, fluoxetine, or paroxetine
  • antifungals, such as voriconazole
  • antiplatelets, such as clopidogrel or ticagrelor
  • beta-blockers, such as acebutolol, atenolol, bisoprolol, or carvedilol
  • bisphosphonates, such as alendronate
  • corticosteroids, such as dexamethasone or prednisone
  • cyclosporine
  • Aspirin Low Strength aspirin
  • diphenhydramine
  • duloxetine
  • omega-3 polyunsaturated fatty acids
  • cyclobenzaprine
  • escitalopram
  • fluticasone  salmeterol
  • betamethasone
  • betaxolol
  • betrixaban
  • bisoprolol
  • captopril
  • carteolol
  • carvedilol
  • celecoxib
  • chlorothiazide
  • deflazacort
  • atorvastatin
  • pregabalin
  • metoprolol
  • esomeprazole
  • acetaminophen
  • hydrocodone
  • ciprofloxacin
  • citalopram
  • clofarabine
  • clomipramine
  • clopidogrel
  • cortisone
  • cyclosporine
  • albuterol
  • montelukast
  • levothyroxine
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D3 (cholecalciferol)
  • alprazolam
  • cetirizine

Pregnancy Category of Nabumetone

  • US FDA pregnancy category: Not assigned

Pregnancy

There is no clinical trial experience with the use of nabumetone during human pregnancy.

  • Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/fetal development. Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after the use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5 %. The risk is believed to increase with the dose and duration of therapy. During the first and second trimester of pregnancy, nabumetone should not be given unless clearly necessary. If nabumetone is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept as low and the duration of treatment as short as possible.

Lactation

  • Because no information is available on the use of nabumetone during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.

Before taking nabumetone,

  • tell your doctor and pharmacist if you are allergic to nabumetone, aspirin, or other NSAIDs such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn), or any other medications. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed in the IMPORTANT WARNING section and any of the following: angiotensin-converting enzymes (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril, enalapril (Vasotec, in Vaseretic), fosinopril, lisinopril (in Zestoretic), moexipril (Univasc), perindopril (Aceon, in Prestalia), quinapril (Accupril, in Quinaretic), ramipril (Altace), and trandolapril (Mavik, in Tarka); angiotensin receptor blockers such as candesartan (Atacand, in Atacand HCT), eprosartan (Teveten), irbesartan (Avapro, in Avalide), losartan (Cozaar, in Hyzaar), olmesartan (Benicar, in Azor, in Benicar HCT, in Tribenzor), telmisartan (Micardis, in Micardis HCT, in Twynsta), and valsartan (in Exforge HCT); medications are taken orally for diabetes; diuretics (‘water pills’); lithium (Lithobid);; phenytoin (Dilantin, Phenytek); and methotrexate (Otrexup, Rasuvo, Trexall). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had asthma, especially if you also have frequent stuffed or runny nose or nasal polyps (swelling of the lining of the nose); heart failure; swelling of the hands, feet, ankles, or lower legs; or kidney or liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant; or are breastfeeding. Nabumetone may harm the fetus and cause problems with delivery if it is taken around 20 weeks or later during pregnancy. Do not take nabumetone around or after 20 weeks of pregnancy, unless you are told to do so by your doctor. If you become pregnant while taking nabumetone, call your doctor.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking nabumetone.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Nabumetone may make your skin sensitive to sunlight.

References’

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Is nabumetone stronger than ibuprofen?

Is nabumetone stronger than ibuprofen?After 12 weeks of treatment, researchers found that nabumetone was similar in effectiveness to ibuprofen and other NSAIDs when treating osteoarthritis. However, the study found that nabumetone was more effective than the other NSAIDs for rheumatoid arthritis.

/Nabumetone is a naphthyl alkenone and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, and analgesic activities. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthyl acetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone. The formation of thromboxane A2, by thromboxane synthase, is also decreased and results in an inhibition of platelet aggregation.

Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.

Nabumetone is a methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthyl acetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, a cyclooxygenase 2 inhibitor, and a prodrug. It is a methoxynaphthalene and a methyl ketone.

Mechanism of Action

Nabumetone’s active metabolite, 6-MNA, is an inhibitor of both COX-1 and COX-2 although it exhibits some COX-2 selectivity.[label, A178903] Inhibition of COX-1 and COX-2 reduces the conversion of arachidonic acid to PGs and thromboxane (TXA2). This reduction in prostanoid production is the common mechanism that mediates the effects of nabumetone. PGE2 is the primary PG involved in the modulation of nociception.[A179023] It mediates peripheral sensitization through a variety of effects.[T116, A179023] PGE2 activates the Gq-coupled EP1 receptor leading to increased activity of the inositol trisphosphate/phospholipase C pathway. Activation of this pathway releases intracellular stores of calcium which directly reduces action potential threshold and activates protein kinase C (PKC) which contributes to several indirect mechanisms. PGE2 also activates the EP4 receptor, coupled to Gs, which activates the adenylyl cyclase/protein kinase A (AC/PKA) signaling pathway. PKA and PKC both contribute to the potentiation of transient receptor potential cation channel subfamily V member 1 (TRPV1) potentiation, which increases sensitivity to heat stimuli. They also activate tetrodotoxin-resistant sodium channels and inhibit inward potassium currents. PKA further contributes to the activation of the P2X3 purine receptor and sensitization of T-type calcium channels. The activation and sensitization of depolarizing ion channels and inhibition of inward potassium currents serve to reduce the intensity of stimulus necessary to generate action potentials in nociceptive sensory afferents. PGE2 act via EP3 to increase sensitivity to bradykinin and via EP2 to further increase heat sensitivity. Central sensitization occurs in the dorsal horn of the spinal cord and is mediated by the EP2 receptor which couples to Gs. Pre-synaptically, this receptor increases the release of pro-nociceptive neurotransmitters glutamate, CGRP, and substance P. Post-synaptically it increases the activity of AMPA and NMDA receptors and produces inhibition of inhibitory glycinergic neurons. Together these lead to a reduced threshold of activating, allowing low intensity stimuli to generate pain signals. PGI2 is known to play a role via its Gs-coupled IP receptor although the magnitude of its contribution varies. It has been proposed to be of greater importance in painful inflammatory conditions such as arthritis. By limiting sensitization, both peripheral and central, via these pathways NSAIDs can effectively reduce inflammatory pain. PGI2 and PGE2 contribute to acute inflammation via their IP and EP2 receptors.[T116, A179044] Similarly to β adrenergic receptors these are Gs-coupled and mediate vasodilation through the AC/PKA pathway. PGE2 also contributes by increasing leukocyte adhesion to the endothelium and attracts the cells to the site of injury.[T116] PGD2 plays a role in the activation of endothelial cell release of cytokines through its DP1 receptor.[A179044] PGI2 and PGE2 modulate T-helper cell activation and differentiation through IP, EP2, and EP4 receptors which are believed to be an important activity in the pathology of arthritic conditions. By limiting the production of these PGs at the site of injury, NSAIDs can reduce inflammation. PGE2 can cross the blood-brain barrier and act on excitatory Gq EP3 receptors on thermoregulatory neurons in the hypothalamus.[T116] This activation triggers an increase in heat generation and a reduction in heat loss to produce a fever. NSAIDs prevent the generation of PGE2 thereby reducing the activity of these neurons. The adverse effects of NSAIDs stem from the protective and regulatory roles of prostanoids which have been well-characterized.[T116] PGI2 and PGE2 regulate blood flow to the kidney by similar mechanisms to the vasodilation they produce in inflammation. Prevention of this regulation by NSAIDs produces vasoconstriction which limits renal function by reducing blood flow and hydrostatic pressure which drives filtration. PGE2 also regulates gastric protection via EP3 receptors which are, in this location, coupled to Gi which inhibits the AC/PKA pathway. This reduces the secretion of protons by H+/K+ ATPase in parietal cells and increases the secretion of mucus and HCO3– by superficial endothelial cells. Disruption of this protective action by NSAIDs leads to ulceration of the gastric mucosa. Lastly, disruption of PGI2, which opposes platelet aggregation, generation by COX-2 selective agents leads to an imbalance with TXA2 generated by COX-1, which promotes aggregation of platelets, leading to increased risk of thrombosis. Since nabumetone is somewhat COX-2 selective it is thought to promote this imbalance and increase thrombotic risk.

Indications of Nabumetone 

  • Indicated for  Symptomatic relief in rheumatoid arthritis.
  • Symptomatic relief in osteoarthritis.
  • Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.
  • Back Pain
  • Sciatica
  • Muscle Pain
  • Rheumatoid Arthritis
  • Frozen Shoulder

Contraindications of Nabumetone

  • Hypersensitivity to the active substance or to any of the excipients,
  • Nabumetone must not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking acetylsalicylic acid or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
  • Nabumetone is contraindicated in patients with severe hepatic failure.
  • Nabumetone is contraindicated in patients with a history of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
  • Nabumetone is contraindicated in patients with active, or history of recurrent, peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
  • Nabumetone is contraindicated in the third trimester of pregnancy and in nursing mothers.
  • Nabumetone is contraindicated in patients with severe heart failure, and in patients with current cerebrovascular or another hemorrhage.
  • a heart attack
  • chronic heart failure
  • abnormal bleeding in the brain resulting in damage to brain tissue, called a hemorrhagic stroke
  • a blood clot
  • an ulcer from too much stomach acid
  • stomach or intestinal ulcer
  • liver problems
  • bleeding of the stomach or intestines
  • kidney transplant
  • pregnancy
  • a rupture in the wall of the stomach or intestine
  • tobacco smoking
  • increased cardiovascular event risk
  • the time immediately after coronary bypass surgery
  • chronic kidney disease stage 4 (severe)
  • chronic kidney disease stage 5 (failure)
  • kidney disease with likely reduction in kidney function
  • aspirin-exacerbated respiratory disease
  • history of gastric bypass surgery
  • history of kidney donation

Dosage of Nabumetone

  • Strengths: 500 mg; 750 mg; 1000 mg

Osteoarthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Rheumatoid Arthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Renal Dose Adjustments

  • Mild renal dysfunction (CrCl 50 mL/min or greater): No adjustment recommended.

Moderate renal dysfunction (CrCl 30 to 49 mL/min)

  • Initial dose: 750 mg orally once a day
  • Maximum dose: 1500 mg/day

Severe renal dysfunction (CrCl less than 30 mL/min)

  • Initial dose: 500 mg orally once a day
  • Maximum dose: 1000 mg/day

Side Effects of Nabumetone

The Most Common

  • shortness of breath (even with mild exertion);
  • swelling or rapid weight gain;
  • the first sign of any skin rash, no matter how mild;
  • signs of stomach bleeding–bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
  • liver problems–nausea, upper stomach pain, itching, tired feeling, flu-like symptoms, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • kidney problems–little or no urinating, painful or difficult urination, swelling in your feet or ankles, feeling tired or short of breath; or
  • low red blood cells (anemia)–pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet.
  • stomach pain, indigestion, nausea;
  • diarrhea, constipation, gas;
  • swelling in your hands and feet;
  • headache, dizziness;
  • itching, skin rash; or
  • ringing in your ears.

Common

  • Acid or sour stomach
  • belching
  • loss of appetite
  • muscle pain
  • pain in lower back or side
  • pinpoint red spots on skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips or tongue
  • rapid breathing
  • red irritated eyes
  • red skin lesions, often with a purple center
  • redness or other discoloration of skin
  • severe or continuing stomach pain
  • bloated full feeling
  • continuing ringing or buzzing or other unexplained noise in ears
  • excess air or gas in stomach or intestines
  • hearing loss
  • indigestion
  • mild diarrhea
  • passing gas

Rare

  • Increased sweating
  • sleepiness or unusual drowsiness
  • sleeplessness
  • trouble sleeping
  • unable to sleep
  • Bleeding gums
  • blistering, peeling, loosening of skin
  • bloody or black, tarry stools
  • bloody or cloudy urine
  • burning upper abdominal pain
  • changes in vision
  • chest pain
  • chills
  • clay-colored stools
  • general feeling of tiredness or weakness
  • greatly decreased frequency of urination or amount of urine
  • high blood pressure
  • hives or welts
  • increased sensitivity of skin to sunlight
  • increased thirst
  • joint pain, stiffness, or swelling
  • large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs

Drug Interactions of Nabumetone

Common medications that may interact with nabumetone include:

  • All other NSAID drugs except nabumetone
  • ACE inhibitors or ARBs, such as captopril, enalapril, or losartan
  • aminoglycosides, such as gentamicin
  • antibiotics, such as ciprofloxacin, norfloxacin, or vancomycin
  • anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
  • antidepressants, such as citalopram, escitalopram, fluoxetine, or paroxetine
  • antifungals, such as voriconazole
  • antiplatelets, such as clopidogrel or ticagrelor
  • beta-blockers, such as acebutolol, atenolol, bisoprolol, or carvedilol
  • bisphosphonates, such as alendronate
  • corticosteroids, such as dexamethasone or prednisone
  • cyclosporine
  • Aspirin Low Strength aspirin
  • diphenhydramine
  • duloxetine
  • omega-3 polyunsaturated fatty acids
  • cyclobenzaprine
  • escitalopram
  • fluticasone  salmeterol
  • betamethasone
  • betaxolol
  • betrixaban
  • bisoprolol
  • captopril
  • carteolol
  • carvedilol
  • celecoxib
  • chlorothiazide
  • deflazacort
  • atorvastatin
  • pregabalin
  • metoprolol
  • esomeprazole
  • acetaminophen
  • hydrocodone
  • ciprofloxacin
  • citalopram
  • clofarabine
  • clomipramine
  • clopidogrel
  • cortisone
  • cyclosporine
  • albuterol
  • montelukast
  • levothyroxine
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D3 (cholecalciferol)
  • alprazolam
  • cetirizine

Pregnancy Category of Nabumetone

  • US FDA pregnancy category: Not assigned

Pregnancy

There is no clinical trial experience with the use of nabumetone during human pregnancy.

  • Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/fetal development. Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after the use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5 %. The risk is believed to increase with the dose and duration of therapy. During the first and second trimester of pregnancy, nabumetone should not be given unless clearly necessary. If nabumetone is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept as low and the duration of treatment as short as possible.

Lactation

  • Because no information is available on the use of nabumetone during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.

Before taking nabumetone,

  • tell your doctor and pharmacist if you are allergic to nabumetone, aspirin, or other NSAIDs such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn), or any other medications. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed in the IMPORTANT WARNING section and any of the following: angiotensin-converting enzymes (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril, enalapril (Vasotec, in Vaseretic), fosinopril, lisinopril (in Zestoretic), moexipril (Univasc), perindopril (Aceon, in Prestalia), quinapril (Accupril, in Quinaretic), ramipril (Altace), and trandolapril (Mavik, in Tarka); angiotensin receptor blockers such as candesartan (Atacand, in Atacand HCT), eprosartan (Teveten), irbesartan (Avapro, in Avalide), losartan (Cozaar, in Hyzaar), olmesartan (Benicar, in Azor, in Benicar HCT, in Tribenzor), telmisartan (Micardis, in Micardis HCT, in Twynsta), and valsartan (in Exforge HCT); medications are taken orally for diabetes; diuretics (‘water pills’); lithium (Lithobid);; phenytoin (Dilantin, Phenytek); and methotrexate (Otrexup, Rasuvo, Trexall). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had asthma, especially if you also have frequent stuffed or runny nose or nasal polyps (swelling of the lining of the nose); heart failure; swelling of the hands, feet, ankles, or lower legs; or kidney or liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant; or are breastfeeding. Nabumetone may harm the fetus and cause problems with delivery if it is taken around 20 weeks or later during pregnancy. Do not take nabumetone around or after 20 weeks of pregnancy, unless you are told to do so by your doctor. If you become pregnant while taking nabumetone, call your doctor.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking nabumetone.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Nabumetone may make your skin sensitive to sunlight.

References’

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Nabumetone 500 mg Oral Tablets – Uses, Dosage, Warning

Nabumetone 500 mg Oral Tablets/Nabumetone is a naphthyl alkenone and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, and analgesic activities. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthyl acetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone. The formation of thromboxane A2, by thromboxane synthase, is also decreased and results in an inhibition of platelet aggregation.

Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.

Nabumetone is a methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthyl acetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, a cyclooxygenase 2 inhibitor, and a prodrug. It is a methoxynaphthalene and a methyl ketone.

Mechanism of Action

Nabumetone’s active metabolite, 6-MNA, is an inhibitor of both COX-1 and COX-2 although it exhibits some COX-2 selectivity.[label, A178903] Inhibition of COX-1 and COX-2 reduces the conversion of arachidonic acid to PGs and thromboxane (TXA2). This reduction in prostanoid production is the common mechanism that mediates the effects of nabumetone. PGE2 is the primary PG involved in the modulation of nociception.[A179023] It mediates peripheral sensitization through a variety of effects.[T116, A179023] PGE2 activates the Gq-coupled EP1 receptor leading to increased activity of the inositol trisphosphate/phospholipase C pathway. Activation of this pathway releases intracellular stores of calcium which directly reduces action potential threshold and activates protein kinase C (PKC) which contributes to several indirect mechanisms. PGE2 also activates the EP4 receptor, coupled to Gs, which activates the adenylyl cyclase/protein kinase A (AC/PKA) signaling pathway. PKA and PKC both contribute to the potentiation of transient receptor potential cation channel subfamily V member 1 (TRPV1) potentiation, which increases sensitivity to heat stimuli. They also activate tetrodotoxin-resistant sodium channels and inhibit inward potassium currents. PKA further contributes to the activation of the P2X3 purine receptor and sensitization of T-type calcium channels. The activation and sensitization of depolarizing ion channels and inhibition of inward potassium currents serve to reduce the intensity of stimulus necessary to generate action potentials in nociceptive sensory afferents. PGE2 act via EP3 to increase sensitivity to bradykinin and via EP2 to further increase heat sensitivity. Central sensitization occurs in the dorsal horn of the spinal cord and is mediated by the EP2 receptor which couples to Gs. Pre-synaptically, this receptor increases the release of pro-nociceptive neurotransmitters glutamate, CGRP, and substance P. Post-synaptically it increases the activity of AMPA and NMDA receptors and produces inhibition of inhibitory glycinergic neurons. Together these lead to a reduced threshold of activating, allowing low intensity stimuli to generate pain signals. PGI2 is known to play a role via its Gs-coupled IP receptor although the magnitude of its contribution varies. It has been proposed to be of greater importance in painful inflammatory conditions such as arthritis. By limiting sensitization, both peripheral and central, via these pathways NSAIDs can effectively reduce inflammatory pain. PGI2 and PGE2 contribute to acute inflammation via their IP and EP2 receptors.[T116, A179044] Similarly to β adrenergic receptors these are Gs-coupled and mediate vasodilation through the AC/PKA pathway. PGE2 also contributes by increasing leukocyte adhesion to the endothelium and attracts the cells to the site of injury.[T116] PGD2 plays a role in the activation of endothelial cell release of cytokines through its DP1 receptor.[A179044] PGI2 and PGE2 modulate T-helper cell activation and differentiation through IP, EP2, and EP4 receptors which are believed to be an important activity in the pathology of arthritic conditions. By limiting the production of these PGs at the site of injury, NSAIDs can reduce inflammation. PGE2 can cross the blood-brain barrier and act on excitatory Gq EP3 receptors on thermoregulatory neurons in the hypothalamus.[T116] This activation triggers an increase in heat generation and a reduction in heat loss to produce a fever. NSAIDs prevent the generation of PGE2 thereby reducing the activity of these neurons. The adverse effects of NSAIDs stem from the protective and regulatory roles of prostanoids which have been well-characterized.[T116] PGI2 and PGE2 regulate blood flow to the kidney by similar mechanisms to the vasodilation they produce in inflammation. Prevention of this regulation by NSAIDs produces vasoconstriction which limits renal function by reducing blood flow and hydrostatic pressure which drives filtration. PGE2 also regulates gastric protection via EP3 receptors which are, in this location, coupled to Gi which inhibits the AC/PKA pathway. This reduces the secretion of protons by H+/K+ ATPase in parietal cells and increases the secretion of mucus and HCO3– by superficial endothelial cells. Disruption of this protective action by NSAIDs leads to ulceration of the gastric mucosa. Lastly, disruption of PGI2, which opposes platelet aggregation, generation by COX-2 selective agents leads to an imbalance with TXA2 generated by COX-1, which promotes aggregation of platelets, leading to increased risk of thrombosis. Since nabumetone is somewhat COX-2 selective it is thought to promote this imbalance and increase thrombotic risk.

Indications of Nabumetone 

  • Indicated for  Symptomatic relief in rheumatoid arthritis.
  • Symptomatic relief in osteoarthritis.
  • Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.
  • Back Pain
  • Sciatica
  • Muscle Pain
  • Rheumatoid Arthritis
  • Frozen Shoulder

Contraindications of Nabumetone

  • Hypersensitivity to the active substance or to any of the excipients,
  • Nabumetone must not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking acetylsalicylic acid or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
  • Nabumetone is contraindicated in patients with severe hepatic failure.
  • Nabumetone is contraindicated in patients with a history of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
  • Nabumetone is contraindicated in patients with active, or history of recurrent, peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
  • Nabumetone is contraindicated in the third trimester of pregnancy and in nursing mothers.
  • Nabumetone is contraindicated in patients with severe heart failure, and in patients with current cerebrovascular or another hemorrhage.
  • a heart attack
  • chronic heart failure
  • abnormal bleeding in the brain resulting in damage to brain tissue, called a hemorrhagic stroke
  • a blood clot
  • an ulcer from too much stomach acid
  • stomach or intestinal ulcer
  • liver problems
  • bleeding of the stomach or intestines
  • kidney transplant
  • pregnancy
  • a rupture in the wall of the stomach or intestine
  • tobacco smoking
  • increased cardiovascular event risk
  • the time immediately after coronary bypass surgery
  • chronic kidney disease stage 4 (severe)
  • chronic kidney disease stage 5 (failure)
  • kidney disease with likely reduction in kidney function
  • aspirin-exacerbated respiratory disease
  • history of gastric bypass surgery
  • history of kidney donation

Dosage of Nabumetone

  • Strengths: 500 mg; 750 mg; 1000 mg

Osteoarthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Rheumatoid Arthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Renal Dose Adjustments

  • Mild renal dysfunction (CrCl 50 mL/min or greater): No adjustment recommended.

Moderate renal dysfunction (CrCl 30 to 49 mL/min)

  • Initial dose: 750 mg orally once a day
  • Maximum dose: 1500 mg/day

Severe renal dysfunction (CrCl less than 30 mL/min)

  • Initial dose: 500 mg orally once a day
  • Maximum dose: 1000 mg/day

Side Effects of Nabumetone

The Most Common

  • shortness of breath (even with mild exertion);
  • swelling or rapid weight gain;
  • the first sign of any skin rash, no matter how mild;
  • signs of stomach bleeding–bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
  • liver problems–nausea, upper stomach pain, itching, tired feeling, flu-like symptoms, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • kidney problems–little or no urinating, painful or difficult urination, swelling in your feet or ankles, feeling tired or short of breath; or
  • low red blood cells (anemia)–pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet.
  • stomach pain, indigestion, nausea;
  • diarrhea, constipation, gas;
  • swelling in your hands and feet;
  • headache, dizziness;
  • itching, skin rash; or
  • ringing in your ears.

Common

  • Acid or sour stomach
  • belching
  • loss of appetite
  • muscle pain
  • pain in lower back or side
  • pinpoint red spots on skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips or tongue
  • rapid breathing
  • red irritated eyes
  • red skin lesions, often with a purple center
  • redness or other discoloration of skin
  • severe or continuing stomach pain
  • bloated full feeling
  • continuing ringing or buzzing or other unexplained noise in ears
  • excess air or gas in stomach or intestines
  • hearing loss
  • indigestion
  • mild diarrhea
  • passing gas

Rare

  • Increased sweating
  • sleepiness or unusual drowsiness
  • sleeplessness
  • trouble sleeping
  • unable to sleep
  • Bleeding gums
  • blistering, peeling, loosening of skin
  • bloody or black, tarry stools
  • bloody or cloudy urine
  • burning upper abdominal pain
  • changes in vision
  • chest pain
  • chills
  • clay-colored stools
  • general feeling of tiredness or weakness
  • greatly decreased frequency of urination or amount of urine
  • high blood pressure
  • hives or welts
  • increased sensitivity of skin to sunlight
  • increased thirst
  • joint pain, stiffness, or swelling
  • large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs

Drug Interactions of Nabumetone

Common medications that may interact with nabumetone include:

  • All other NSAID drugs except nabumetone
  • ACE inhibitors or ARBs, such as captopril, enalapril, or losartan
  • aminoglycosides, such as gentamicin
  • antibiotics, such as ciprofloxacin, norfloxacin, or vancomycin
  • anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
  • antidepressants, such as citalopram, escitalopram, fluoxetine, or paroxetine
  • antifungals, such as voriconazole
  • antiplatelets, such as clopidogrel or ticagrelor
  • beta-blockers, such as acebutolol, atenolol, bisoprolol, or carvedilol
  • bisphosphonates, such as alendronate
  • corticosteroids, such as dexamethasone or prednisone
  • cyclosporine
  • Aspirin Low Strength aspirin
  • diphenhydramine
  • duloxetine
  • omega-3 polyunsaturated fatty acids
  • cyclobenzaprine
  • escitalopram
  • fluticasone  salmeterol
  • betamethasone
  • betaxolol
  • betrixaban
  • bisoprolol
  • captopril
  • carteolol
  • carvedilol
  • celecoxib
  • chlorothiazide
  • deflazacort
  • atorvastatin
  • pregabalin
  • metoprolol
  • esomeprazole
  • acetaminophen
  • hydrocodone
  • ciprofloxacin
  • citalopram
  • clofarabine
  • clomipramine
  • clopidogrel
  • cortisone
  • cyclosporine
  • albuterol
  • montelukast
  • levothyroxine
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D3 (cholecalciferol)
  • alprazolam
  • cetirizine

Pregnancy Category of Nabumetone

  • US FDA pregnancy category: Not assigned

Pregnancy

There is no clinical trial experience with the use of nabumetone during human pregnancy.

  • Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/fetal development. Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after the use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5 %. The risk is believed to increase with the dose and duration of therapy. During the first and second trimester of pregnancy, nabumetone should not be given unless clearly necessary. If nabumetone is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept as low and the duration of treatment as short as possible.

Lactation

  • Because no information is available on the use of nabumetone during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.

Before taking nabumetone,

  • tell your doctor and pharmacist if you are allergic to nabumetone, aspirin, or other NSAIDs such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn), or any other medications. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed in the IMPORTANT WARNING section and any of the following: angiotensin-converting enzymes (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril, enalapril (Vasotec, in Vaseretic), fosinopril, lisinopril (in Zestoretic), moexipril (Univasc), perindopril (Aceon, in Prestalia), quinapril (Accupril, in Quinaretic), ramipril (Altace), and trandolapril (Mavik, in Tarka); angiotensin receptor blockers such as candesartan (Atacand, in Atacand HCT), eprosartan (Teveten), irbesartan (Avapro, in Avalide), losartan (Cozaar, in Hyzaar), olmesartan (Benicar, in Azor, in Benicar HCT, in Tribenzor), telmisartan (Micardis, in Micardis HCT, in Twynsta), and valsartan (in Exforge HCT); medications are taken orally for diabetes; diuretics (‘water pills’); lithium (Lithobid);; phenytoin (Dilantin, Phenytek); and methotrexate (Otrexup, Rasuvo, Trexall). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had asthma, especially if you also have frequent stuffed or runny nose or nasal polyps (swelling of the lining of the nose); heart failure; swelling of the hands, feet, ankles, or lower legs; or kidney or liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant; or are breastfeeding. Nabumetone may harm the fetus and cause problems with delivery if it is taken around 20 weeks or later during pregnancy. Do not take nabumetone around or after 20 weeks of pregnancy, unless you are told to do so by your doctor. If you become pregnant while taking nabumetone, call your doctor.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking nabumetone.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Nabumetone may make your skin sensitive to sunlight.

References’

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Nabumetone 500 mg Tablets – Indications, Contraindications

Nabumetone 500 mg Tablets/Nabumetone is a naphthyl alkenone and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, and analgesic activities. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthyl acetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone. The formation of thromboxane A2, by thromboxane synthase, is also decreased and results in an inhibition of platelet aggregation.

Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.

Nabumetone is a methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthyl acetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, a cyclooxygenase 2 inhibitor, and a prodrug. It is a methoxynaphthalene and a methyl ketone.

Mechanism of Action

Nabumetone’s active metabolite, 6-MNA, is an inhibitor of both COX-1 and COX-2 although it exhibits some COX-2 selectivity.[label, A178903] Inhibition of COX-1 and COX-2 reduces the conversion of arachidonic acid to PGs and thromboxane (TXA2). This reduction in prostanoid production is the common mechanism that mediates the effects of nabumetone. PGE2 is the primary PG involved in the modulation of nociception.[A179023] It mediates peripheral sensitization through a variety of effects.[T116, A179023] PGE2 activates the Gq-coupled EP1 receptor leading to increased activity of the inositol trisphosphate/phospholipase C pathway. Activation of this pathway releases intracellular stores of calcium which directly reduces action potential threshold and activates protein kinase C (PKC) which contributes to several indirect mechanisms. PGE2 also activates the EP4 receptor, coupled to Gs, which activates the adenylyl cyclase/protein kinase A (AC/PKA) signaling pathway. PKA and PKC both contribute to the potentiation of transient receptor potential cation channel subfamily V member 1 (TRPV1) potentiation, which increases sensitivity to heat stimuli. They also activate tetrodotoxin-resistant sodium channels and inhibit inward potassium currents. PKA further contributes to the activation of the P2X3 purine receptor and sensitization of T-type calcium channels. The activation and sensitization of depolarizing ion channels and inhibition of inward potassium currents serve to reduce the intensity of stimulus necessary to generate action potentials in nociceptive sensory afferents. PGE2 act via EP3 to increase sensitivity to bradykinin and via EP2 to further increase heat sensitivity. Central sensitization occurs in the dorsal horn of the spinal cord and is mediated by the EP2 receptor which couples to Gs. Pre-synaptically, this receptor increases the release of pro-nociceptive neurotransmitters glutamate, CGRP, and substance P. Post-synaptically it increases the activity of AMPA and NMDA receptors and produces inhibition of inhibitory glycinergic neurons. Together these lead to a reduced threshold of activating, allowing low intensity stimuli to generate pain signals. PGI2 is known to play a role via its Gs-coupled IP receptor although the magnitude of its contribution varies. It has been proposed to be of greater importance in painful inflammatory conditions such as arthritis. By limiting sensitization, both peripheral and central, via these pathways NSAIDs can effectively reduce inflammatory pain. PGI2 and PGE2 contribute to acute inflammation via their IP and EP2 receptors.[T116, A179044] Similarly to β adrenergic receptors these are Gs-coupled and mediate vasodilation through the AC/PKA pathway. PGE2 also contributes by increasing leukocyte adhesion to the endothelium and attracts the cells to the site of injury.[T116] PGD2 plays a role in the activation of endothelial cell release of cytokines through its DP1 receptor.[A179044] PGI2 and PGE2 modulate T-helper cell activation and differentiation through IP, EP2, and EP4 receptors which are believed to be an important activity in the pathology of arthritic conditions. By limiting the production of these PGs at the site of injury, NSAIDs can reduce inflammation. PGE2 can cross the blood-brain barrier and act on excitatory Gq EP3 receptors on thermoregulatory neurons in the hypothalamus.[T116] This activation triggers an increase in heat generation and a reduction in heat loss to produce a fever. NSAIDs prevent the generation of PGE2 thereby reducing the activity of these neurons. The adverse effects of NSAIDs stem from the protective and regulatory roles of prostanoids which have been well-characterized.[T116] PGI2 and PGE2 regulate blood flow to the kidney by similar mechanisms to the vasodilation they produce in inflammation. Prevention of this regulation by NSAIDs produces vasoconstriction which limits renal function by reducing blood flow and hydrostatic pressure which drives filtration. PGE2 also regulates gastric protection via EP3 receptors which are, in this location, coupled to Gi which inhibits the AC/PKA pathway. This reduces the secretion of protons by H+/K+ ATPase in parietal cells and increases the secretion of mucus and HCO3– by superficial endothelial cells. Disruption of this protective action by NSAIDs leads to ulceration of the gastric mucosa. Lastly, disruption of PGI2, which opposes platelet aggregation, generation by COX-2 selective agents leads to an imbalance with TXA2 generated by COX-1, which promotes aggregation of platelets, leading to increased risk of thrombosis. Since nabumetone is somewhat COX-2 selective it is thought to promote this imbalance and increase thrombotic risk.

Indications of Nabumetone 

  • Indicated for  Symptomatic relief in rheumatoid arthritis.
  • Symptomatic relief in osteoarthritis.
  • Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.
  • Back Pain
  • Sciatica
  • Muscle Pain
  • Rheumatoid Arthritis
  • Frozen Shoulder

Contraindications of Nabumetone

  • Hypersensitivity to the active substance or to any of the excipients,
  • Nabumetone must not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking acetylsalicylic acid or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
  • Nabumetone is contraindicated in patients with severe hepatic failure.
  • Nabumetone is contraindicated in patients with a history of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
  • Nabumetone is contraindicated in patients with active, or history of recurrent, peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
  • Nabumetone is contraindicated in the third trimester of pregnancy and in nursing mothers.
  • Nabumetone is contraindicated in patients with severe heart failure, and in patients with current cerebrovascular or another hemorrhage.
  • a heart attack
  • chronic heart failure
  • abnormal bleeding in the brain resulting in damage to brain tissue, called a hemorrhagic stroke
  • a blood clot
  • an ulcer from too much stomach acid
  • stomach or intestinal ulcer
  • liver problems
  • bleeding of the stomach or intestines
  • kidney transplant
  • pregnancy
  • a rupture in the wall of the stomach or intestine
  • tobacco smoking
  • increased cardiovascular event risk
  • the time immediately after coronary bypass surgery
  • chronic kidney disease stage 4 (severe)
  • chronic kidney disease stage 5 (failure)
  • kidney disease with likely reduction in kidney function
  • aspirin-exacerbated respiratory disease
  • history of gastric bypass surgery
  • history of kidney donation

Dosage of Nabumetone

  • Strengths: 500 mg; 750 mg; 1000 mg

Osteoarthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Rheumatoid Arthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Renal Dose Adjustments

  • Mild renal dysfunction (CrCl 50 mL/min or greater): No adjustment recommended.

Moderate renal dysfunction (CrCl 30 to 49 mL/min)

  • Initial dose: 750 mg orally once a day
  • Maximum dose: 1500 mg/day

Severe renal dysfunction (CrCl less than 30 mL/min)

  • Initial dose: 500 mg orally once a day
  • Maximum dose: 1000 mg/day

Side Effects of Nabumetone

The Most Common

  • shortness of breath (even with mild exertion);
  • swelling or rapid weight gain;
  • the first sign of any skin rash, no matter how mild;
  • signs of stomach bleeding–bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
  • liver problems–nausea, upper stomach pain, itching, tired feeling, flu-like symptoms, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • kidney problems–little or no urinating, painful or difficult urination, swelling in your feet or ankles, feeling tired or short of breath; or
  • low red blood cells (anemia)–pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet.
  • stomach pain, indigestion, nausea;
  • diarrhea, constipation, gas;
  • swelling in your hands and feet;
  • headache, dizziness;
  • itching, skin rash; or
  • ringing in your ears.

Common

  • Acid or sour stomach
  • belching
  • loss of appetite
  • muscle pain
  • pain in lower back or side
  • pinpoint red spots on skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips or tongue
  • rapid breathing
  • red irritated eyes
  • red skin lesions, often with a purple center
  • redness or other discoloration of skin
  • severe or continuing stomach pain
  • bloated full feeling
  • continuing ringing or buzzing or other unexplained noise in ears
  • excess air or gas in stomach or intestines
  • hearing loss
  • indigestion
  • mild diarrhea
  • passing gas

Rare

  • Increased sweating
  • sleepiness or unusual drowsiness
  • sleeplessness
  • trouble sleeping
  • unable to sleep
  • Bleeding gums
  • blistering, peeling, loosening of skin
  • bloody or black, tarry stools
  • bloody or cloudy urine
  • burning upper abdominal pain
  • changes in vision
  • chest pain
  • chills
  • clay-colored stools
  • general feeling of tiredness or weakness
  • greatly decreased frequency of urination or amount of urine
  • high blood pressure
  • hives or welts
  • increased sensitivity of skin to sunlight
  • increased thirst
  • joint pain, stiffness, or swelling
  • large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs

Drug Interactions of Nabumetone

Common medications that may interact with nabumetone include:

  • All other NSAID drugs except nabumetone
  • ACE inhibitors or ARBs, such as captopril, enalapril, or losartan
  • aminoglycosides, such as gentamicin
  • antibiotics, such as ciprofloxacin, norfloxacin, or vancomycin
  • anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
  • antidepressants, such as citalopram, escitalopram, fluoxetine, or paroxetine
  • antifungals, such as voriconazole
  • antiplatelets, such as clopidogrel or ticagrelor
  • beta-blockers, such as acebutolol, atenolol, bisoprolol, or carvedilol
  • bisphosphonates, such as alendronate
  • corticosteroids, such as dexamethasone or prednisone
  • cyclosporine
  • Aspirin Low Strength aspirin
  • diphenhydramine
  • duloxetine
  • omega-3 polyunsaturated fatty acids
  • cyclobenzaprine
  • escitalopram
  • fluticasone  salmeterol
  • betamethasone
  • betaxolol
  • betrixaban
  • bisoprolol
  • captopril
  • carteolol
  • carvedilol
  • celecoxib
  • chlorothiazide
  • deflazacort
  • atorvastatin
  • pregabalin
  • metoprolol
  • esomeprazole
  • acetaminophen
  • hydrocodone
  • ciprofloxacin
  • citalopram
  • clofarabine
  • clomipramine
  • clopidogrel
  • cortisone
  • cyclosporine
  • albuterol
  • montelukast
  • levothyroxine
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D3 (cholecalciferol)
  • alprazolam
  • cetirizine

Pregnancy Category of Nabumetone

  • US FDA pregnancy category: Not assigned

Pregnancy

There is no clinical trial experience with the use of nabumetone during human pregnancy.

  • Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/fetal development. Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after the use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5 %. The risk is believed to increase with the dose and duration of therapy. During the first and second trimester of pregnancy, nabumetone should not be given unless clearly necessary. If nabumetone is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept as low and the duration of treatment as short as possible.

Lactation

  • Because no information is available on the use of nabumetone during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.

Before taking nabumetone,

  • tell your doctor and pharmacist if you are allergic to nabumetone, aspirin, or other NSAIDs such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn), or any other medications. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed in the IMPORTANT WARNING section and any of the following: angiotensin-converting enzymes (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril, enalapril (Vasotec, in Vaseretic), fosinopril, lisinopril (in Zestoretic), moexipril (Univasc), perindopril (Aceon, in Prestalia), quinapril (Accupril, in Quinaretic), ramipril (Altace), and trandolapril (Mavik, in Tarka); angiotensin receptor blockers such as candesartan (Atacand, in Atacand HCT), eprosartan (Teveten), irbesartan (Avapro, in Avalide), losartan (Cozaar, in Hyzaar), olmesartan (Benicar, in Azor, in Benicar HCT, in Tribenzor), telmisartan (Micardis, in Micardis HCT, in Twynsta), and valsartan (in Exforge HCT); medications are taken orally for diabetes; diuretics (‘water pills’); lithium (Lithobid);; phenytoin (Dilantin, Phenytek); and methotrexate (Otrexup, Rasuvo, Trexall). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had asthma, especially if you also have frequent stuffed or runny nose or nasal polyps (swelling of the lining of the nose); heart failure; swelling of the hands, feet, ankles, or lower legs; or kidney or liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant; or are breastfeeding. Nabumetone may harm the fetus and cause problems with delivery if it is taken around 20 weeks or later during pregnancy. Do not take nabumetone around or after 20 weeks of pregnancy, unless you are told to do so by your doctor. If you become pregnant while taking nabumetone, call your doctor.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking nabumetone.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Nabumetone may make your skin sensitive to sunlight.

References’

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Nabumetone – Uses, Dosage, Side Effects, Interactions

Nabumetone is a naphthyl alkenone and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, antipyretic, and analgesic activities. Nabumetone is a prodrug that upon hepatic catalysis converts into the active moiety 6-methoxy-2-naphthyl acetic acid (6MNA). 6MNA inhibits the activity of the enzymes cyclo-oxygenase I and II, resulting in decreased formation of precursors of prostaglandins and thromboxanes. The resulting decrease in prostaglandin synthesis is responsible for the therapeutic effects of nabumetone. The formation of thromboxane A2, by thromboxane synthase, is also decreased and results in an inhibition of platelet aggregation.

Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.

Nabumetone is a methyl ketone that is 2-butanone in which one of the methyl hydrogens at position 4 is replaced by a 6-methoxy-2-naphthyl group. A prodrug that is converted to the active metabolite, 6-methoxy-2-naphthyl acetic acid, following oral administration. It is shown to have a slightly lower risk of gastrointestinal side effects than most other non-steroidal anti-inflammatory drugs. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, a cyclooxygenase 2 inhibitor, and a prodrug. It is a methoxynaphthalene and a methyl ketone.

Mechanism of Action

Nabumetone’s active metabolite, 6-MNA, is an inhibitor of both COX-1 and COX-2 although it exhibits some COX-2 selectivity.[label, A178903] Inhibition of COX-1 and COX-2 reduces the conversion of arachidonic acid to PGs and thromboxane (TXA2). This reduction in prostanoid production is the common mechanism that mediates the effects of nabumetone. PGE2 is the primary PG involved in the modulation of nociception.[A179023] It mediates peripheral sensitization through a variety of effects.[T116, A179023] PGE2 activates the Gq-coupled EP1 receptor leading to increased activity of the inositol trisphosphate/phospholipase C pathway. Activation of this pathway releases intracellular stores of calcium which directly reduces action potential threshold and activates protein kinase C (PKC) which contributes to several indirect mechanisms. PGE2 also activates the EP4 receptor, coupled to Gs, which activates the adenylyl cyclase/protein kinase A (AC/PKA) signaling pathway. PKA and PKC both contribute to the potentiation of transient receptor potential cation channel subfamily V member 1 (TRPV1) potentiation, which increases sensitivity to heat stimuli. They also activate tetrodotoxin-resistant sodium channels and inhibit inward potassium currents. PKA further contributes to the activation of the P2X3 purine receptor and sensitization of T-type calcium channels. The activation and sensitization of depolarizing ion channels and inhibition of inward potassium currents serve to reduce the intensity of stimulus necessary to generate action potentials in nociceptive sensory afferents. PGE2 act via EP3 to increase sensitivity to bradykinin and via EP2 to further increase heat sensitivity. Central sensitization occurs in the dorsal horn of the spinal cord and is mediated by the EP2 receptor which couples to Gs. Pre-synaptically, this receptor increases the release of pro-nociceptive neurotransmitters glutamate, CGRP, and substance P. Post-synaptically it increases the activity of AMPA and NMDA receptors and produces inhibition of inhibitory glycinergic neurons. Together these lead to a reduced threshold of activating, allowing low intensity stimuli to generate pain signals. PGI2 is known to play a role via its Gs-coupled IP receptor although the magnitude of its contribution varies. It has been proposed to be of greater importance in painful inflammatory conditions such as arthritis. By limiting sensitization, both peripheral and central, via these pathways NSAIDs can effectively reduce inflammatory pain. PGI2 and PGE2 contribute to acute inflammation via their IP and EP2 receptors.[T116, A179044] Similarly to β adrenergic receptors these are Gs-coupled and mediate vasodilation through the AC/PKA pathway. PGE2 also contributes by increasing leukocyte adhesion to the endothelium and attracts the cells to the site of injury.[T116] PGD2 plays a role in the activation of endothelial cell release of cytokines through its DP1 receptor.[A179044] PGI2 and PGE2 modulate T-helper cell activation and differentiation through IP, EP2, and EP4 receptors which are believed to be an important activity in the pathology of arthritic conditions. By limiting the production of these PGs at the site of injury, NSAIDs can reduce inflammation. PGE2 can cross the blood-brain barrier and act on excitatory Gq EP3 receptors on thermoregulatory neurons in the hypothalamus.[T116] This activation triggers an increase in heat generation and a reduction in heat loss to produce a fever. NSAIDs prevent the generation of PGE2 thereby reducing the activity of these neurons. The adverse effects of NSAIDs stem from the protective and regulatory roles of prostanoids which have been well-characterized.[T116] PGI2 and PGE2 regulate blood flow to the kidney by similar mechanisms to the vasodilation they produce in inflammation. Prevention of this regulation by NSAIDs produces vasoconstriction which limits renal function by reducing blood flow and hydrostatic pressure which drives filtration. PGE2 also regulates gastric protection via EP3 receptors which are, in this location, coupled to Gi which inhibits the AC/PKA pathway. This reduces the secretion of protons by H+/K+ ATPase in parietal cells and increases the secretion of mucus and HCO3– by superficial endothelial cells. Disruption of this protective action by NSAIDs leads to ulceration of the gastric mucosa. Lastly, disruption of PGI2, which opposes platelet aggregation, generation by COX-2 selective agents leads to an imbalance with TXA2 generated by COX-1, which promotes aggregation of platelets, leading to increased risk of thrombosis. Since nabumetone is somewhat COX-2 selective it is thought to promote this imbalance and increase thrombotic risk.

Indications of Nabumetone 

  • Indicated for  Symptomatic relief in rheumatoid arthritis.
  • Symptomatic relief in osteoarthritis.
  • Nabumetone is a long-acting nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used in the therapy of chronic arthritis. Nabumetone has been linked to rare instances of clinically apparent, idiosyncratic drug-induced liver disease.
  • Back Pain
  • Sciatica
  • Muscle Pain
  • Rheumatoid Arthritis
  • Frozen Shoulder

Contraindications of Nabumetone

  • Hypersensitivity to the active substance or to any of the excipients,
  • Nabumetone must not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking acetylsalicylic acid or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients.
  • Nabumetone is contraindicated in patients with severe hepatic failure.
  • Nabumetone is contraindicated in patients with a history of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.
  • Nabumetone is contraindicated in patients with active, or history of recurrent, peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
  • Nabumetone is contraindicated in the third trimester of pregnancy and in nursing mothers.
  • Nabumetone is contraindicated in patients with severe heart failure, and in patients with current cerebrovascular or another hemorrhage.
  • a heart attack
  • chronic heart failure
  • abnormal bleeding in the brain resulting in damage to brain tissue, called a hemorrhagic stroke
  • a blood clot
  • an ulcer from too much stomach acid
  • stomach or intestinal ulcer
  • liver problems
  • bleeding of the stomach or intestines
  • kidney transplant
  • pregnancy
  • a rupture in the wall of the stomach or intestine
  • tobacco smoking
  • increased cardiovascular event risk
  • the time immediately after coronary bypass surgery
  • chronic kidney disease stage 4 (severe)
  • chronic kidney disease stage 5 (failure)
  • kidney disease with likely reduction in kidney function
  • aspirin-exacerbated respiratory disease
  • history of gastric bypass surgery
  • history of kidney donation

Dosage of Nabumetone

  • Strengths: 500 mg; 750 mg; 1000 mg

Osteoarthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Rheumatoid Arthritis

  • Initial dose: 1000 mg orally once a day
  • Maintenance dose: 1500 to 2000 mg orally per day in 1 or 2 divided doses
  • Maximum dose: 2000 mg/day

Renal Dose Adjustments

  • Mild renal dysfunction (CrCl 50 mL/min or greater): No adjustment recommended.

Moderate renal dysfunction (CrCl 30 to 49 mL/min)

  • Initial dose: 750 mg orally once a day
  • Maximum dose: 1500 mg/day

Severe renal dysfunction (CrCl less than 30 mL/min)

  • Initial dose: 500 mg orally once a day
  • Maximum dose: 1000 mg/day

Side Effects of Nabumetone

The Most Common

  • shortness of breath (even with mild exertion);
  • swelling or rapid weight gain;
  • the first sign of any skin rash, no matter how mild;
  • signs of stomach bleeding–bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
  • liver problems–nausea, upper stomach pain, itching, tired feeling, flu-like symptoms, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
  • kidney problems–little or no urinating, painful or difficult urination, swelling in your feet or ankles, feeling tired or short of breath; or
  • low red blood cells (anemia)–pale skin, unusual tiredness, feeling light-headed or short of breath, cold hands and feet.
  • stomach pain, indigestion, nausea;
  • diarrhea, constipation, gas;
  • swelling in your hands and feet;
  • headache, dizziness;
  • itching, skin rash; or
  • ringing in your ears.

Common

  • Acid or sour stomach
  • belching
  • loss of appetite
  • muscle pain
  • pain in lower back or side
  • pinpoint red spots on skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips or tongue
  • rapid breathing
  • red irritated eyes
  • red skin lesions, often with a purple center
  • redness or other discoloration of skin
  • severe or continuing stomach pain
  • bloated full feeling
  • continuing ringing or buzzing or other unexplained noise in ears
  • excess air or gas in stomach or intestines
  • hearing loss
  • indigestion
  • mild diarrhea
  • passing gas

Rare

  • Increased sweating
  • sleepiness or unusual drowsiness
  • sleeplessness
  • trouble sleeping
  • unable to sleep
  • Bleeding gums
  • blistering, peeling, loosening of skin
  • bloody or black, tarry stools
  • bloody or cloudy urine
  • burning upper abdominal pain
  • changes in vision
  • chest pain
  • chills
  • clay-colored stools
  • general feeling of tiredness or weakness
  • greatly decreased frequency of urination or amount of urine
  • high blood pressure
  • hives or welts
  • increased sensitivity of skin to sunlight
  • increased thirst
  • joint pain, stiffness, or swelling
  • large, hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs

Drug Interactions of Nabumetone

Common medications that may interact with nabumetone include:

  • All other NSAID drugs except nabumetone
  • ACE inhibitors or ARBs, such as captopril, enalapril, or losartan
  • aminoglycosides, such as gentamicin
  • antibiotics, such as ciprofloxacin, norfloxacin, or vancomycin
  • anticoagulants (blood thinners) such as apixaban, dabigatran, fondaparinux, heparin, or warfarin
  • antidepressants, such as citalopram, escitalopram, fluoxetine, or paroxetine
  • antifungals, such as voriconazole
  • antiplatelets, such as clopidogrel or ticagrelor
  • beta-blockers, such as acebutolol, atenolol, bisoprolol, or carvedilol
  • bisphosphonates, such as alendronate
  • corticosteroids, such as dexamethasone or prednisone
  • cyclosporine
  • Aspirin Low Strength aspirin
  • diphenhydramine
  • duloxetine
  • omega-3 polyunsaturated fatty acids
  • cyclobenzaprine
  • escitalopram
  • fluticasone  salmeterol
  • betamethasone
  • betaxolol
  • betrixaban
  • bisoprolol
  • captopril
  • carteolol
  • carvedilol
  • celecoxib
  • chlorothiazide
  • deflazacort
  • atorvastatin
  • pregabalin
  • metoprolol
  • esomeprazole
  • acetaminophen
  • hydrocodone
  • ciprofloxacin
  • citalopram
  • clofarabine
  • clomipramine
  • clopidogrel
  • cortisone
  • cyclosporine
  • albuterol
  • montelukast
  • levothyroxine
  • Vitamin B12 (cyanocobalamin)
  • Vitamin C (ascorbic acid)
  • Vitamin D3 (cholecalciferol)
  • alprazolam
  • cetirizine

Pregnancy Category of Nabumetone

  • US FDA pregnancy category: Not assigned

Pregnancy

There is no clinical trial experience with the use of nabumetone during human pregnancy.

  • Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/fetal development. Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after the use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5 %. The risk is believed to increase with the dose and duration of therapy. During the first and second trimester of pregnancy, nabumetone should not be given unless clearly necessary. If nabumetone is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept as low and the duration of treatment as short as possible.

Lactation

  • Because no information is available on the use of nabumetone during breastfeeding, other agents may be preferred, especially while nursing a newborn or preterm infant.

Before taking nabumetone,

  • tell your doctor and pharmacist if you are allergic to nabumetone, aspirin, or other NSAIDs such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn), or any other medications. Ask your doctor or pharmacist for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed in the IMPORTANT WARNING section and any of the following: angiotensin-converting enzymes (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril, enalapril (Vasotec, in Vaseretic), fosinopril, lisinopril (in Zestoretic), moexipril (Univasc), perindopril (Aceon, in Prestalia), quinapril (Accupril, in Quinaretic), ramipril (Altace), and trandolapril (Mavik, in Tarka); angiotensin receptor blockers such as candesartan (Atacand, in Atacand HCT), eprosartan (Teveten), irbesartan (Avapro, in Avalide), losartan (Cozaar, in Hyzaar), olmesartan (Benicar, in Azor, in Benicar HCT, in Tribenzor), telmisartan (Micardis, in Micardis HCT, in Twynsta), and valsartan (in Exforge HCT); medications are taken orally for diabetes; diuretics (‘water pills’); lithium (Lithobid);; phenytoin (Dilantin, Phenytek); and methotrexate (Otrexup, Rasuvo, Trexall). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • tell your doctor if you have or have ever had asthma, especially if you also have frequent stuffed or runny nose or nasal polyps (swelling of the lining of the nose); heart failure; swelling of the hands, feet, ankles, or lower legs; or kidney or liver disease.
  • tell your doctor if you are pregnant, plan to become pregnant; or are breastfeeding. Nabumetone may harm the fetus and cause problems with delivery if it is taken around 20 weeks or later during pregnancy. Do not take nabumetone around or after 20 weeks of pregnancy, unless you are told to do so by your doctor. If you become pregnant while taking nabumetone, call your doctor.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking nabumetone.
  • plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Nabumetone may make your skin sensitive to sunlight.

References’

 

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Scopolamine Hydrobromide – Uses, Dosage, Side Effects, Interaction

Scopolamine Hydrobromide is the hydrobromide salt form of scopolamine, a tropane alkaloid derived from plants of the nightshade family (Solanaceae), specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic, and antivertigo properties. Structurally similar to acetylcholine, scopolamine antagonizes acetylcholine activity mediated by muscarinic receptors located on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. The agent is used to cause mydriasis, cycloplegia, to control the secretion of saliva and gastric acid, to slow gut motility, and prevent vomiting.

Scopolamine is a tropane alkaloid derived from plants of the nightshade family (Solanaceae), specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties. Structurally similar to acetylcholine, scopolamine antagonizes acetylcholine activity mediated by muscarinic receptors located on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. The agent is used to cause mydriasis, cycloplegia, to control the secretion of saliva and gastric acid, to slow gut motility, and prevent vomiting.

Scopolamine is a natural plant alkaloid that has potent anticholinergic effects and is used to treat mild to moderate nausea, motion sickness and allergic rhinitis. Scopolamine has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.[rx]

Mechanism of Action

Acetylcholine (ACh) is a neurotransmitter that can signal through ligand-gated cation channels (nicotinic receptors) and G-protein-coupled muscarinic receptors (mAChRs). ACh signaling via mAChRs located in the central nervous system (CNS) and periphery can regulate smooth muscle contraction, glandular secretions, heart rate, and various neurological phenomena such as learning and memory.[rx,rx] mAChRs can be divided into five subtypes, M1-M5, expressed at various levels throughout the brain.[rx] Also, M2 receptors are found in the heart and M3 receptors in smooth muscles, mediating effects apart from the direct modulation of the parasympathetic nervous system.[rx] While M1, M3, and M5 mAChRs primarily couple to Gq proteins to activate phospholipase C, M2 and M4 mainly couple to Gi/o proteins to inhibit adenylyl cyclase and modulate cellular ion flow.[rx] This system, in part, helps to control physiological responses such as nausea and vomiting.[rx]

Scopolamine acts as a non-selective competitive inhibitor of M1-M5 mAChRs, albeit with weaker M5 inhibition; as such, scopolamine is an anticholinergic with various dose-dependent therapeutic and adverse effects.[rx,rx] The exact mechanism(s) of action of scopolamine remains poorly understood. Recent evidence suggests that M1 (and possibly M2) mAChR antagonism at interneurons acts through inhibition of downstream neurotransmitter release and subsequent pyramidal neuron activation to mediate neurological responses associated with stress and depression.[rx] Similar antagonism of M4 and M5 receptors is associated with potential therapeutic benefits in neurological conditions such as schizophrenia and substance abuse disorders.[rx] The significance of these observations to scopolamine’s current therapeutic indications of preventing nausea and vomiting is unclear but is linked to its anticholinergic effect and ability to alter signaling through the CNS associated with vomiting.[rx,rx]

Indications of Scopolamine Hydrobromide

  • Motion sickness
  • Nausea- vomiting, 
  • Travel sickness or motion sickness
  • Vertigo, dizziness, Drowsiness
  • Gastrointestinal tract spasm, Genitourinary spasm
  • IBS (irritable bowel syndrome)
  • Postoperative nausea and vomiting
  • Parkinsonian Tremor
  • Adjuvants, Anesthesia – Agents that are administered in association with anesthetics to increase effectiveness, improve delivery, or decrease the required dosage.
  • Cholinergic Antagonists – Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.
  • Muscarinic antagonists – Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
  • Mydriatics agents – that dilate the pupil. They may be either sympathomimetics or parasympatholytics. Since little of the medication crosses the blood-brain barrier, this drug has less effect on the brain and therefore causes a reduced occurrence of the centrally-mediated effects (such as delusions, somnolence, and inhibition of motor functions) which reduce the usefulness of some other anticholinergic drugs.
  • Hyoscine butyl bromide or Scopolamine – is still capable of affecting the chemoreceptor trigger zone, due to the lack of a well-developed blood-brain-barrier in the medulla oblongata, which increases the antiemetic effect it produces via local action on the smooth muscle of the gastrointestinal tract.[rx]

Contraindications of Scopolamine Hydrobromide

  • Myasthenia gravis, narrow-angle glaucoma, tachycardia, megacolon; hypersensitivity
  • Hyoscine should not be administered to patients with myasthenia gravis, megacolon, angle-closure glaucoma, tachycardia, prostatic enlargement with urinary retention, gastrointestinal obstruction, mechanical stenosis in the region of the gastrointestinal tract, or paralytic ileus.
  • Hyoscine should not be given by intramuscular injection to patients being treated with anticoagulant drugs since intramuscular hematoma may occur.
  • Hypersensitivity to this drug
  • Allergy
  • Depression
  • Porphyria

Dosage of Scopolamine Hydrobromide

Strengths: 1.5 mg; 1 mg/mL; 1 mg/72 hr; 0.4 mg/mL; 0.4 mg

  • Nausea/Vomiting – Post-operative nausea and vomiting (PONV): Apply 1 patch to the hairless area behind the ear the evening before a scheduled surgery.
  • Motion Sickness – Apply 1 patch to the hairless area behind the ear at least 4 hours before the antiemetic effect is needed

Side Effects Of Scopolamine Hydrobromide

The most common
  • Symptoms of exposure to this chemical include drowsiness, sleepiness, excitement, hallucinations, delirium, psychotic behavior and central nervous system depression.
  • Other symptoms include narcosis, mydriasis, dryness of the mouth and restlessness.
  • Drowsiness
  • Dry mouth
  • Headache
  • Indigestion
  • Depression
  • Skin rashes
  • Restlessness
  • Weight gain
  • Mydriasis, cycloplegia, eye pruritus.
  • Muscle weakness.
  • Urinary retention, dysuria.
  • Flushing, sweating, dry skin, rash, erythema, pruritus, skin burns, contact dermatitis (transdermal).

Common

Serious

Drug Interactions of Scopolamine Hydrobromide

Scopolamine may interact with the following drugs

Due to interactions with the metabolism of other drugs, hyoscine can cause significant unwanted side effects when taken with other medications. Specific attention should be paid to other medications in the same pharmacologic class as hyoscine, also known as anticholinergics. These medications could potentially interact with the metabolism of hyoscine:

Pregnancy & Lactation Of Scopolamine Hydrobromide

 FDA Pregnancy Category –  C

Pregnancy

The safety of  Scopolamine Hydrobromide in human pregnancy has not been established although studies in animals have not demonstrated teratogenic effects. As with other drugs, it is not advisable to administer  Scopolamine Hydrobromide in pregnancy.

Lactation

There are no data on the excretion of  Scopolamine Hydrobromide in human breast milk. Taking Hyoscine Hydrobromide whilst breastfeeding is not recommended.

What special precautions should I follow?

Before using scopolamine patches,

  • tell your doctor and pharmacist if you are allergic to scopolamine, other belladonna alkaloids, any other medications, or any of the ingredients in scopolamine patches. Ask your doctor or pharmacist, check the package label, or check the Medication Guide for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: antihistamines such as meclizine (Antivert, Bonine, others); medications for anxiety, irritable bowel disease, motion sickness, pain, Parkinson’s disease, seizures or urinary problems; muscle relaxants; sedatives; sleeping pills; tranquilizers; or tricyclic antidepressants such as desipramine (Norpramin), clomipramine (Anafranil), imipramine (Tofranil), and trimipramine (Surmontil) Many other medications may also interact with scopolamine patch, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • tell your doctor if you have angle-closure glaucoma (a condition where the fluid is suddenly blocked and unable to flow out of the eye causing a quick, severe increase in eye pressure which may lead to a loss of vision). Your doctor will probably tell you not to use a scopolamine patch.
  • tell your doctor if you have or have ever had open-angle glaucoma (increase in internal eye pressure that damages the optic nerve); seizures; psychotic disorders (conditions that cause difficulty telling the difference between things or ideas that are real and things or ideas that are not real); stomach or intestinal obstruction; difficulty urinating; preeclampsia (a condition during pregnancy with increased blood pressure, high protein levels in the urine, or organ problems); or heart, liver, or kidney disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while using scopolamine patches, call your doctor immediately.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are using scopolamine patches.
  • you should know that a scopolamine patch may make you drowsy. Do not drive a car or operate machinery until you know how scopolamine patches will affect you. If you participate in water sports, use caution because this medication can have disorienting effects.
  • talk to your doctor about the safe use of alcoholic beverages while using this medication. Alcohol can make the side effects caused by scopolamine patches worse.
  • talk to your doctor about the risks and benefits of using scopolamine if you are 65 years of age or older. Older adults should not usually use scopolamine because it is not as safe or effective as other medications that can be used to treat the same condition.[rx]

References

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Scopolamine – Uses, Dosage, Side Effects, Interactions

Scopolamine is a tropane alkaloid isolated from members of the Solanaceae family of plants, similar to atropine and hyoscyamine, all of which structurally mimic the natural neurotransmitter acetylcholine.[rx,rx]

Scopolamine Hydrobromide is the hydrobromide salt form of scopolamine, a tropane alkaloid derived from plants of the nightshade family (Solanaceae), specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties. Structurally similar to acetylcholine, scopolamine antagonizes acetylcholine activity mediated by muscarinic receptors located on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. The agent is used to cause mydriasis, cycloplegia, to control the secretion of saliva and gastric acid, to slow gut motility, and prevent vomiting.

Scopolamine is a tropane alkaloid derived from plants of the nightshade family (Solanaceae), specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties. Structurally similar to acetylcholine, scopolamine antagonizes acetylcholine activity mediated by muscarinic receptors located on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. The agent is used to cause mydriasis, cycloplegia, to control the secretion of saliva and gastric acid, to slow gut motility, and prevent vomiting.

Scopolamine is a natural plant alkaloid that has potent anticholinergic effects and is used to treat mild to moderate nausea, motion sickness and allergic rhinitis. Scopolamine has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.[rx]

Mechanism of action

Acetylcholine (ACh) is a neurotransmitter that can signal through ligand-gated cation channels (nicotinic receptors) and G-protein-coupled muscarinic receptors (mAChRs). ACh signaling via mAChRs located in the central nervous system (CNS) and periphery can regulate smooth muscle contraction, glandular secretions, heart rate, and various neurological phenomena such as learning and memory.[rx,rx] mAChRs can be divided into five subtypes, M1-M5, expressed at various levels throughout the brain.[rx] Also, M2 receptors are found in the heart and M3 receptors in smooth muscles, mediating effects apart from the direct modulation of the parasympathetic nervous system.[rx] While M1, M3, and M5 mAChRs primarily couple to Gq proteins to activate phospholipase C, M2 and M4 mainly couple to Gi/o proteins to inhibit adenylyl cyclase and modulate cellular ion flow.[rx] This system, in part, helps to control physiological responses such as nausea and vomiting.[rx]

Scopolamine acts as a non-selective competitive inhibitor of M1-M5 mAChRs, albeit with weaker M5 inhibition; as such, scopolamine is an anticholinergic with various dose-dependent therapeutic and adverse effects.[rx,rx] The exact mechanism(s) of action of scopolamine remains poorly understood. Recent evidence suggests that M1 (and possibly M2) mAChR antagonism at interneurons acts through inhibition of downstream neurotransmitter release and subsequent pyramidal neuron activation to mediate neurological responses associated with stress and depression.[rx] Similar antagonism of M4 and M5 receptors is associated with potential therapeutic benefits in neurological conditions such as schizophrenia and substance abuse disorders.[rx] The significance of these observations to scopolamine’s current therapeutic indications of preventing nausea and vomiting is unclear but is linked to its anticholinergic effect and ability to alter signalling through the CNS associated with vomiting.[rx,rx]

Indications of Scopolamine

  • Motion sickness
  • Nausea- vomiting, 
  • Travel sickness or motion sickness
  • Vertigo, dizziness, Drowsiness
  • Gastrointestinal tract spasm, Genitourinary spasm
  • IBS (irritable bowel syndrome)
  • Postoperative nausea and vomiting
  • Parkinsonian Tremor
  • Adjuvants, Anesthesia – Agents that are administered in association with anesthetics to increase effectiveness, improve delivery, or decrease the required dosage.
  • Cholinergic Antagonists – Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.
  • Muscarinic antagonists – Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
  • Mydriatics agents – that dilate the pupil. They may be either sympathomimetics or parasympatholytics.
  • Since little of the medication crosses the blood-brain barrier, this drug has less effect on the brain and therefore causes a reduced occurrence of the centrally-mediated effects (such as delusions, somnolence, and inhibition of motor functions) which reduce the usefulness of some other anticholinergic drugs.
  • Hyoscine butyl bromide or Scopolamine – is still capable of affecting the chemoreceptor trigger zone, due to the lack of a well-developed blood-brain-barrier in the medulla oblongata, which increases the antiemetic effect it produces via local action on the smooth muscle of the gastrointestinal tract.[rx]

Contraindications of Scopolamine

  • Myasthenia gravis, narrow-angle glaucoma, tachycardia, megacolon; hypersensitivity
  • Hyoscine should not be administered to patients with myasthenia gravis, megacolon, angle-closure glaucoma, tachycardia, prostatic enlargement with urinary retention, gastrointestinal obstruction, mechanical stenosis in the region of the gastrointestinal tract, or paralytic ileus.
  • Hyoscine should not be given by intramuscular injection to patients being treated with anticoagulant drugs since intramuscular hematoma may occur.
  • Hypersensitivity to this drug
  • Allergy
  • Depression
  • Porphyria

Dosage of Scopolamine

Strengths: 1.5 mg; 1 mg/mL; 1 mg/72 hr; 0.4 mg/mL; 0.4 mg

  • Nausea/Vomiting – Post-operative nausea and vomiting (PONV): Apply 1 patch to the hairless area behind the ear the evening before a scheduled surgery.
  • Motion Sickness – Apply 1 patch to the hairless area behind the ear at least 4 hours before the antiemetic effect is needed

Side Effects Of Scopolamine

The most common
  • Symptoms of exposure to this chemical include drowsiness, sleepiness, excitement, hallucinations, delirium, psychotic behavior and central nervous system depression.
  • Other symptoms include narcosis, mydriasis, dryness of the mouth and restlessness.
  • Drowsiness
  • Dry mouth
  • Headache
  • Indigestion
  • Depression
  • Skin rashes
  • Restlessness
  • Weight gain
  • Mydriasis, cycloplegia, eye pruritus.
  • Muscle weakness.
  • Urinary retention, dysuria.
  • Flushing, sweating, dry skin, rash, erythema, pruritus, skin burns, contact dermatitis (transdermal).

Common

Serious

Drug Interactions of Scopolamine

Scopolamine may interact with the following drugs

Due to interactions with the metabolism of other drugs, hyoscine can cause significant unwanted side effects when taken with other medications. Specific attention should be paid to other medications in the same pharmacologic class as hyoscine, also known as anticholinergics. These medications could potentially interact with the metabolism of hyoscine: analgesics/pain medications, ethanol, zolpidem, thiazide diuretics, buprenorphine, anticholinergic drugs such as tiotropium, etc.[rx]

Pregnancy & Lactation Of Scopolamine

 FDA Pregnancy Category C

Pregnancy

The safety of Hyoscine Hydrobromide in human pregnancy has not been established although studies in animals have not demonstrated teratogenic effects. As with other drugs, it is not advisable to administer Hyoscine Hydrobromide in pregnancy.

Lactation

There are no data on the excretion of Hyoscine Hydrobromide in human breast milk. Taking Hyoscine Hydrobromide whilst breastfeeding is not recommended.

What special precautions should I follow?

Before using scopolamine patches,

  • tell your doctor and pharmacist if you are allergic to scopolamine, other belladonna alkaloids, any other medications, or any of the ingredients in scopolamine patches. Ask your doctor or pharmacist, check the package label, or check the Medication Guide for a list of the ingredients.
  • tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: antihistamines such as meclizine (Antivert, Bonine, others); medications for anxiety, irritable bowel disease, motion sickness, pain, Parkinson’s disease, seizures or urinary problems; muscle relaxants; sedatives; sleeping pills; tranquilizers; or tricyclic antidepressants such as desipramine (Norpramin), clomipramine (Anafranil), imipramine (Tofranil), and trimipramine (Surmontil) Many other medications may also interact with scopolamine patch, so be sure to tell your doctor about all the medications you are taking, even those that do not appear on this list.
  • tell your doctor if you have angle-closure glaucoma (a condition where the fluid is suddenly blocked and unable to flow out of the eye causing a quick, severe increase in eye pressure which may lead to a loss of vision). Your doctor will probably tell you not to use a scopolamine patch.
  • tell your doctor if you have or have ever had open-angle glaucoma (increase in internal eye pressure that damages the optic nerve); seizures; psychotic disorders (conditions that cause difficulty telling the difference between things or ideas that are real and things or ideas that are not real); stomach or intestinal obstruction; difficulty urinating; preeclampsia (a condition during pregnancy with increased blood pressure, high protein levels in the urine, or organ problems); or heart, liver, or kidney disease.
  • tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while using scopolamine patches, call your doctor immediately.
  • if you are having surgery, including dental surgery, tell the doctor or dentist that you are using scopolamine patches.
  • you should know that a scopolamine patch may make you drowsy. Do not drive a car or operate machinery until you know how scopolamine patches will affect you. If you participate in water sports, use caution because this medication can have disorienting effects.
  • talk to your doctor about the safe use of alcoholic beverages while using this medication. Alcohol can make the side effects caused by scopolamine patches worse.
  • talk to your doctor about the risks and benefits of using scopolamine if you are 65 years of age or older. Older adults should not usually use scopolamine because it is not as safe or effective as other medications that can be used to treat the same condition.[rx]

References

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Hyoscine – Uses, Dosage, Side Effects, Interactions

Hyoscine or Scopolamine hydrobromide appears as colorless crystals or white powder or solid. Has no odor. pH (of 5% solution): 4-5.5. Slightly efflorescent in dry air. Bitter, acrid taste.

Scopolamine Hydrobromide is the hydrobromide salt form of scopolamine, a tropane alkaloid derived from plants of the nightshade family (Solanaceae), specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic, and antivertigo properties. Structurally similar to acetylcholine, scopolamine antagonizes acetylcholine activity mediated by muscarinic receptors located on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. The agent is used to cause mydriasis, cycloplegia, to control the secretion of saliva and gastric acid, to slow gut motility, and prevent vomiting.

Scopolamine hydrobromide appears as colorless crystals or white powder or solid. Has no odor. pH (of 5% solution): 4-5.5. Slightly efflorescent in dry air. Bitter, acrid taste. (NTP, 1992). Scopolamine hydrobromide (anhydrous) is a hydrobromide that is obtained by the reaction of scopolamine with hydrogen bromide. It has a role as a muscarinic antagonist. It contains scopolamine(1+).

Mechanism Of Actions

Scopolamine Hydrobromide is the hydrobromide salt form of scopolamine, a tropane alkaloid derived from plants of the nightshade family (Solanaceae), specifically Hyoscyamus niger and Atropa belladonna, with anticholinergic, antiemetic and antivertigo properties. Structurally similar to acetylcholine, scopolamine antagonizes acetylcholine activity mediated by muscarinic receptors located on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. The agent is used to cause mydriasis, cycloplegia, to control the secretion of saliva and gastric acid, to slow gut motility, and prevent vomiting.

Indications of Hyoscine Hydrobromide

  • Motion sickness, Vertigo
  • Nausea- vomiting, 
  • Travel sickness or motion sickness
  • Vertigo, dizziness, Drowsiness
  • Gastrointestinal tract spasm, Genitourinary spasm
  • IBS (irritable bowel syndrome)
  • Postoperative nausea and vomiting
  • Adjuvants, Anesthesia – Agents that are administered in association with anesthetics to increase effectiveness, improve delivery, or decrease the required dosage.
  • Cholinergic Antagonists – Drugs that bind to but do not activate CHOLINERGIC RECEPTORS, thereby blocking the actions of ACETYLCHOLINE or cholinergic agonists.
  • Muscarinic antagonists – Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
  • Mydriatics agents – that dilate the pupil. They may be either sympathomimetics or parasympatholytics.
  • Since little of the medication crosses the blood-brain barrier, this drug has less effect on the brain and therefore causes a reduced occurrence of the centrally-mediated effects (such as delusions, somnolence, and inhibition of motor functions) which reduce the usefulness of some other anticholinergic drugs.
  • Hyoscine butyl bromide – is still capable of affecting the chemoreceptor trigger zone, due to the lack of a well-developed blood-brain-barrier in the medulla oblongata, which increases the antiemetic effect it produces via local action on the smooth muscle of the gastrointestinal tract.[rx]

Contraindications of Hyoscine Hydrobromide

  • Myasthenia gravis, narrow-angle glaucoma, tachycardia, megacolon; hypersensitivity
  • Hyoscine should not be administered to patients with myasthenia gravis, megacolon, angle-closure glaucoma, tachycardia, prostatic enlargement with urinary retention, gastrointestinal obstruction, mechanical stenosis in the region of the gastrointestinal tract, or paralytic ileus.
  • Hyoscine should not be given by intramuscular injection to patients being treated with anticoagulant drugs since intramuscular hematoma may occur.
  • Hypersensitivity to this drug
  • Allergy
  • Depression
  • Porphyria

Dosage of Hyoscine Hydrobromide

Strength: 150mg, 300mg

Dosage by tablet strength

Dosage for hyoscine hydrobromide tablets (150 or 300 micrograms)
Age Which strength? Dose
4 to 9 years 150 micrograms half tablet to 1 tablet
10 to 17 years 150 micrograms 1 tablet to 2 tablets
10 to 17 years 300 micrograms half tablet to 1 tablet
18 years and over 300 micrograms 1 tablet

How to take tablets for excess saliva

  • These tablets are available on prescription only. They can be taken by adults and children aged 12 years or older.
  • The usual dose is 1 tablet (300 micrograms), 3 times a day.

How to use patches for excess saliva

Adults and children aged 10 years or older:

  • Stick a patch to the skin behind the ear.
  • Leave the patch on for 72 hours (3 days).
  • After 72 hours, remove the patch.
  • Stick a new patch behind the other ear.
  • After 72 hours, remove the patch.
  • Repeat the process.

Occasionally a doctor may prescribe patches for a child under the age of 9 years. In this case, they’ll use your child’s weight to work out what size patch to use. They may only need to use half a patch.

How to use patches for travel sickness

Patches are suitable for adults and children aged 10 years or older.

  • Stick a patch to the skin behind the ear 5 to 6 hours before the start of your journey (or the evening before you travel).
  • Remove the patch at the end of your journey.
  • For long journeys, you can keep the patch on for up to 72 hours (3 days).
  • If you’re still traveling after 72 hours, remove the first patch and stick a new patch behind the other ear. You can keep this on for another 72 hours if needed.

Oral
Gastrointestinal tract spasm, Genitourinary spasm

  • Adult: As hyoscine butyl bromide: 20 mg 4 times daily.
  • Child: As hyoscine butyl bromide: 6-11 years 10 mg tid; ≥12 years Same as adult dose.

Oral
Prophylaxis of motion sickness

  • Adult: As hyoscine hydrobromide: Initially, 0.15-0.3 mg 20-30 minutes before a journey, repeat 6 hourly if needed, up to max 3 doses in 24 hours. Max: 0.9 mg daily.
  • Child: As hyoscine hydrobromide: 3-4 years Initially, 0.075 mg, repeated once if needed. Max: 0.15 mg daily; >4-10 years 0.075-0.15 mg, repeat 6 hourly if needed. Max: 0.45 mg daily; >10 years 0.15-0.30 mg, repeat 6 hourly if needed. Max: 0.9 mg daily. All doses should be given 20-30 minutes before a journey.

Oral
IBS (irritable bowel syndrome)

  • Adult: As hyoscine butyl bromide: Initially, 10 mg tid, may increase up to 20 mg 4 times daily if needed.
  • Child: As hyoscine butyl bromide: 6-11 years 10 mg tid; ≥12 years Same as adult dose.

Parenteral
Motion sickness, Nausea, and vomiting, Vertigo

  • Adult: As hyoscine hydrobromide: 0.2 mg as a single dose via IM or SC inj (may also be given via IV inj if required).
  • Child: As hyoscine hydrobromide: 0.006 mg/kg as a single dose via IM or SC inj.

Parenteral
Gastrointestinal tract spasm, Genitourinary spasm

  • Adult: As hyoscine butyl bromide: 20 mg via slow IV or IM inj, may be repeated after 30 minutes if needed. Max: 100 mg daily.

Parenteral
Preoperative medication

  • Adult: As hyoscine hydrobromide: 0.2-0.6 mg given via IV, IM, or SC inj, 30-60 minutes prior to induction of anesthesia.
  • Child: As hyoscine hydrobromide: 0.015 mg/kg given via IM or SC inj, 30-60 minutes prior to induction of anesthesia.

Transdermal
Prophylaxis of motion sickness

  • Adult: As hyoscine hydrobromide patch containing 1.5 mg: Apply 1 patch behind the ear, 4-6 hours before a journey or in the evening before the journey.
  • Child: >10 years Same as adult dose.

Transdermal
Postoperative nausea and vomiting

  • Adult: As hyoscine hydrobromide patch containing 1.5 mg: Apply 1 patch behind the ear on the evening before the surgery or 1 hour before cesarean section. Discard 24 hours after the surgery.
  • Child: >10 years Same as adult dose.

Side Effects Of Hyoscine Hydrobromide

The most common
  • Symptoms of exposure to this chemical include drowsiness, sleepiness, excitement, hallucinations, delirium, psychotic behavior and central nervous system depression.
  • Other symptoms include narcosis, mydriasis, dryness of the mouth and restlessness.
  • Drowsiness
  • Dry mouth
  • Headache
  • Indigestion
  • Depression
  • Skin rashes
  • Restlessness
  • Weight gain
  • Mydriasis, cycloplegia, eye pruritus.
  • Muscle weakness.
  • Urinary retention, dysuria.
  • Flushing, sweating, dry skin, rash, erythema, pruritus, skin burns, contact dermatitis (transdermal).

Common

Serious

Drug Interactions of Hyoscine Hydrobromide

Hyoscine Hydrobromide may interact with the following drugs

Pregnancy & Lactation Of Hyoscine Hydrobromide

 FDA Pregnancy Category C

Pregnancy

The safety of Hyoscine Hydrobromide in human pregnancy has not been established although studies in animals have not demonstrated teratogenic effects. As with other drugs, it is not advisable to administer Hyoscine Hydrobromide in pregnancy.

Lactation

There are no data on the excretion of Hyoscine Hydrobromide in human breast milk. Taking Hyoscine Hydrobromide whilst breastfeeding is not recommended.

What if I take too much?

Taking 1 extra dose of hyoscine hydrobromide by accident is unlikely to harm you. But you may get more side effects, such as a dry mouth or blurred vision. The amount of hyoscine hydrobromide that can lead to an overdose varies from person to person, and too much hyoscine can be dangerous.

References

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